Bicyclic bridged compounds that contain a nitrogen which has three bonds. The nomenclature indicates the number of atoms in each path around the rings, such as [2.2.2] for three equal length paths. Some members are TROPANES and BETA LACTAMS.
Eight-carbon saturated hydrocarbon group of the methane series. Include isomers and derivatives.
A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)
Quinuclidines are organic compounds consisting of a tricyclic structure with a three-membered ring fused to a piperidine ring, often used as building blocks in the synthesis of pharmaceuticals and bioactive molecules.
N-methyl-8-azabicyclo[3.2.1]octanes best known for the ones found in PLANTS.
'Bicyclo compounds' in medicinal chemistry refer to organic molecules containing two fused rings, where each ring shares two common atoms, creating a topological structure that resembles two overlapping circles or bicycle tires.
Organic compounds composed exclusively of carbon and hydrogen forming a closed ring that may be either alicyclic or aromatic.
Six-carbon saturated hydrocarbon group of the methane series. Include isomers and derivatives. Various polyneuropathies are caused by hexane poisoning.
A class of organic compounds containing two ring structures, one of which is made up of more than one kind of atom, usually carbon plus another atom. The heterocycle may be either aromatic or nonaromatic.
A group of compounds with an 8-carbon ring. They may be saturated or unsaturated.
Isomeric forms and derivatives of octanol (C8H17OH).
'Azā compounds' are a class of organic molecules containing at least one nitrogen atom in a five-membered ring, often found in naturally occurring substances and pharmaceuticals, with the name derived from the Arabic word "azZa" meaning 'strong' referring to the ring's aromatic stability.
A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.
A hemoflagellate subspecies of parasitic protozoa that causes Rhodesian sleeping sickness in humans. It is carried by Glossina pallidipes, G. morsitans and occasionally other species of game-attacking tsetse flies.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
The characteristic three-dimensional shape of a molecule.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.

Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism. (1/173)

Zopiclone is a widely prescribed, nonbenzodiazepine hypnotic that is extensively metabolized by the liver in humans. The aim of the present study was to identify the human cytochrome P-450 (CYP) isoforms involved in zopiclone metabolism in vitro. Zopiclone metabolism was studied with different human liver microsomes and a panel of heterologously expressed human CYPs (CYP1A2, 2C8, 2C9, 2C18, 2C19, 2D6, 2E1, and 3A4). In human liver microsomes, zopiclone was metabolized into N-desmethyl-zopiclone (ND-Z) and N-oxide-zopiclone (NO-Z) with the following K(m) and V(m) of 78 +/- 5 and 84 +/- 19 microM, 45 +/- 1 and 54 +/- 5 pmol/min/mg for ND-Z and NO-Z generation, respectively. Ketoconazole (CYP3A inhibitor) inhibited approximately 40% of the generation of both metabolites, sulfaphenazole (CYP2C inhibitor) inhibited the formation of ND-Z, whereas alpha-naphtoflavone (CYP1A), quinidine (CYP2D6), and chlorzoxazone (CYP2E1) did not affect zopiclone metabolism. The generation of ND-Z and NO-Z were highly correlated to testosterone 6beta-hydroxylation (CYP3A activity, r = 0.95 and 0.92, respectively; p =.0001), and ND-Z was highly correlated to CYP2C8 activity (paclitaxel 6alpha-hydroxylase; r = 0.76, p =.004). Recombinant CYP2C8 had the highest enzymatic activity toward zopiclone metabolism into both its metabolites, followed by CYP2C9 and 3A4. CYP3A4 is the major enzyme involved in zopiclone metabolism in vitro, and CYP2C8 contributes significantly to ND-Z formation.  (+info)

Zopiclone use during pregnancy. (2/173)

QUESTION: One of my patients, whom I had treated with a 2-week course of zopiclone for insomnia, conceived while using the medication. She is concerned. How should I advise her? ANSWER: Based on available, albeit limited, evidence, zopiclone does not appear to be a major human teratogen.  (+info)

Characterization of the interaction of zopiclone with gamma-aminobutyric acid type A receptors. (3/173)

Zopiclone is a cyclopyrrolone that is used clinically as a hypnotic. Although this drug is known to interact with neuronal gamma-aminobutyric acid type A receptors, its binding site(s) within the receptor oligomer has been reported to be distinct from that of the classical benzodiazepines. After photoaffinity labeling with flunitrazepam, receptors in rat cerebellar membranes showed differentially reduced affinity for flunitrazepam and zopiclone by 50- and 3-fold, respectively. Because histidine 101 of the alpha-subunit is a major site of photolabeling, we have made specific substitutions of this residue and studied the consequences on the binding properties of zopiclone and diazepam using recombinant alpha1beta2gamma2-receptors transiently expressed in tsA201 cells. Both compounds showed similar binding profiles with receptors containing mutated alpha-subunits, suggesting a similar interaction with the residue at position 101. At alpha1beta2gamma3-receptors, flunitrazepam affinity was dramatically decreased by approximately 36-fold, whereas the affinity for zopiclone was decreased only 3-fold, suggesting a differential contribution of the gamma-subunit to the binding pocket. Additionally, we used electrophysiological techniques to examine the contribution of the gamma-subunit isoform in the receptor oligomer to ligand recognition using recombinant receptors expressed in Xenopus oocytes. Both compounds are agonists at alpha1beta2gamma2- and alpha1beta2gamma3-receptors, with flunitrazepam being more potent but less efficacious. In summary, these data suggest that histidine 101 of the alpha1-subunit plays a similar role in ligand recognition for zopiclone, diazepam, and flunitrazepam.  (+info)

Mechanism-based pharmacokinetic/pharmacodynamic modeling of the electroencephalogram effects of GABAA receptor modulators: in vitro-in vivo correlations. (4/173)

A mechanism-based pharmacokinetic-pharmacodynamic (PK/PD) model for neuroactive steroids, comprising a separate characterization of 1) the receptor activation process and 2) the stimulus-response relationship, was applied to various nonsteroidal GABAA receptor modulators. The EEG effects of nine prototypical GABAA receptor modulators (six benzodiazepines, one imidazopyridine, one cyclopyrrolone, and one beta-carboline) were determined in rats in conjunction with plasma concentrations. Population PK/PD modeling revealed monophasic concentration-EEG effect relationships with large differences in potency (EC50) and intrinsic activity between the compounds. The data were analyzed on the basis of the mechanism-based PK/PD model for (synthetic) neuroactive steroids on the assumption of a single and unique stimulus-response relationship. The model converged yielding estimates of both the apparent in vivo receptor affinity (KPD) and the in vivo intrinsic efficacy (ePD). The values of KPD ranged from 0.41 +/- 0 ng.ml(-1) for bretazenil to 436 +/- 72 ng.ml(-1) for clobazam and the values for e(PD) from -0.27 +/- 0 for methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate to 0.54 +/- 0.02 for diazepam. Significant linear correlations were observed between KPD for unbound concentrations and the affinity in an in vitro receptor bioassay (r = 0.93) and between e(PD) and the GABA-shift in vitro (r = 0.95). The findings of this investigation show that the in vivo effects of nonsteroidal GABAA receptor modulators and (synthetic) neuroactive steroids can be described on the basis of a single unique transducer function. In this paradigm, the nonsteroidal GABAA receptor modulators behave as partial agonists relative to neuroactive steroids.  (+info)

Effect of zaleplon, a non-benzodiazepine hypnotic, on melatonin secretion in rabbits. (5/173)

Melatonin, a major hormone secreted by the pineal gland, is known to play an important role in regulation of the circadian rhythm. (N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide (zaleplon) is a non-benzodiazepine hypnotic that acts via the benzodiazepine site of the GABA(A) receptor. In the present study, we investigated the effect of zaleplon on melatonin secretion in rabbits using RIA and compared the effect to triazolam and zopiclone. Zaleplon increased a dose-dependent concentration of melatonin in rabbit plasma collected at 30 min after intravenous administration at doses of 1 and 2 mg/kg. The zaleplon-induced increase in plasma melatonin level was not blocked by flumazenil, a benzodiazepine-receptor antagonist. In contrast, triazolam and zopiclone failed to affect the plasma melatonin level. We also investigated the effect of zaleplon on intracellular cAMP in rat pinealocytes. Consequently, zaleplon had no effect on the intracellular cAMP levels in rat pinealocytes. These results of the present studies suggest that zaleplon may promote melatonin secretion and the elevation of plasma levels of melatonin may suggest an influence of zaleplon on chronobiology.  (+info)

Dependence on legal psychotropic drugs among alcoholics. (6/173)

AIMS: Dependence on legal psychotropic drugs (PTD) has been reported to have increased in alcoholics, but previous studies report conflicting results concerning the rate of increase and clinical characteristics. The aim of the present study was first, to assess the dependence rate of PTD among alcoholics in open and institutionalized care, and to compare these populations with the general population, and second, to assess rates and doses of high- and low-dose PTD-dependence among alcoholics. METHODS: In 1997, alcoholics in open and institutionalized care were asked to anonymously fill in a questionnaire on their drug use and dependence. Healthy controls were included. The number of attending subjects was 130 open-care alcoholics at the Department of Alcohol and Drug Diseases in Malmo, Sweden; 23 alcoholics in institutionalized care at Karlsvik Rehabilitation Centre in Hoor, Sweden; and 120 healthy controls at Vardcentralen Kirseberg, a primary health care centre located in a Malmo area. The approximate attendance rate was 75, 70 and 95%, respectively. The questionnaire was based on DSM-IV criteria for dependence. RESULTS: The total rate of PTD-dependent alcoholics was higher in the institutionalized group (35%) than in the open-care setting (14%): difference in proportions (p(1)-p(2) 21%; 95% CI: 1%, 41%). Alcoholics were more often PTD-dependent (17%) than were healthy controls (2%), (p(1)-p(2) 15%; 95% CI: 9%, 21%). Benzodiazepines (BZD) were the most common PTD. Only four out of a total of 23 BZD-dependent alcoholics developed high-dose BZD-dependence. Those subjects were also misusing other drugs, including cannabis. CONCLUSIONS: We conclude that alcoholism is associated with legal PTD-dependence and illegal drug misuse. High-dose BZD-dependence is infrequent among BZD-dependent alcoholics.  (+info)

Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats. (7/173)

The encephalographic (EEG) properties of zaleplon were investigated in comparison with those of other sedative hypnotics in conscious rats with chronically implanted electrodes. The oral administration of zaleplon (0.25-1.0 mg/kg), triazolam (0.0625-0.25 mg/kg), zopiclone (1.0-4.0 mg/kg), brotizolam (0.0625-0.25 mg/kg), and nitrazepam (0.125-0.5 mg/kg) lengthened the total sleep in a dose-dependent manner. On distribution of sleep-wakefulness stages, zaleplon, in particular, increased the slow wave deep sleep (SWDS), whereas triazolam, brotizolam, and nitrazepam increased the slow wave light sleep (SWLS) in a dose-dependent manner. Zopiclone significantly increased the SWDS at a dose of 2 mg/kg and both the SWLS and the SWDS at a dose of 4 mg/kg. All tested hypnotics caused no influence on fast wave sleep (FWS) at doses tested. The appearance of the sleep-inducing activity of zaleplon was more rapid than those of any compounds tested, and zaleplon significantly increased the relative EEG power density in the delta frequency band over that of triazolam at 20 and 30 min after the administration in the spectral analysis. Therefore, the present findings suggest that the non-benzodiazepine zaleplon can be expected to exhibit high practical potential as a hypnotic and is characterized by an increase in SWDS with rapid onset of hypnotic action.  (+info)

Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride). (8/173)

Two novel N-methyl-d-aspartate (NMDA) antagonists with unique chemical structures, EAA-090 (2-[8,9-dioxo-2, 6-diazabicyclo[5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride), were compared with CGS-19755 (Selfotel) in ligand binding, electrophysiology, and neuroprotection assays. CGS-19755, EAA-090 and EAB-318 inhibited [(3)H]3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid binding to NMDA receptors with IC(50) values of 55, 28, and 7.9 nM, respectively. All three compounds decreased the duration of spontaneous synaptic currents and inhibited NMDA-activated currents in rat hippocampal neurons. IC(50) values for inhibition of current induced by 10 microM NMDA were 795, 477, and 69 nM for CGS-19755, EAA-090, and EAB-318, respectively. The NMDA antagonists protected chick embryo retina slices and cultured rat hippocampal and cortical neurons from glutamate- and NMDA-induced neurotoxicity. In experiments in which different NMDA receptor splice variants and subtypes were expressed in Xenopus oocytes, all three antagonists preferentially blocked NMDA-elicited currents mediated by N-methyl-d-aspartate receptor (NR)1 splice variants containing the N-terminal insertion. They also favored NR2A-versus NR2B- or NR2C-containing NMDA receptors, with EAA-090 showing the greatest selectivity. EAA-090 was 10 times more potent at blocking NR2A-versus NR2B- or NR2C-containing NMDA receptors. In addition to being the most potent NMDA antagonist, EAB-318 inhibited alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and kainate receptors. The combination of NMDA and AMPA/kainate block enabled EAB-318 to protect neurons against ischemia induced cell death.  (+info)

Azabicyclo compounds are a type of organic compound that contain at least one nitrogen atom (azacycle) and two rings fused together (bicyclic). The nitrogen atom can be part of either a saturated or unsaturated ring, and the rings themselves can be composed of carbon atoms only or contain other heteroatoms such as oxygen or sulfur.

The term "azabicyclo" is often followed by a set of three numbers that specify the number of atoms in each of the three rings involved in the fusion. For example, azabicyclo[3.2.1]octane is a compound with two fused rings containing 3 and 2 carbon atoms, respectively, and one nitrogen atom forming the third ring of 1 carbon atom.

These compounds have a wide range of applications in pharmaceuticals, agrochemicals, and materials science due to their unique structures and properties. In particular, azabicyclo compounds are often used as building blocks for the synthesis of complex natural products and bioactive molecules.

I'm sorry for any confusion, but "octanes" is not a medical term. It is a term used in chemistry and physics, particularly in reference to fuel. Octane is a hydrocarbon molecule found in gasoline, and it is used as a measure of the fuel's ability to resist engine knocking or pinging during combustion.

The octane rating of gasoline typically ranges from 87 (regular) to 91-93 (premium). Higher-octane fuels are often recommended for high-performance vehicles that have higher compression ratios in their engines. If you have any questions related to medical terminology, I'd be happy to help!

Bicyclo compounds, heterocyclic, refer to a class of organic compounds that contain two rings in their structure, at least one of which is a heterocycle. A heterocycle is a cyclic compound containing atoms of at least two different elements as part of the ring structure. The term "bicyclo" indicates that there are two rings present in the molecule, with at least one common atom between them.

These compounds have significant importance in medicinal chemistry and pharmacology due to their unique structures and properties. They can be found in various natural products and are also synthesized for use as drugs, agrochemicals, and other chemical applications. The heterocyclic rings often contain nitrogen, oxygen, or sulfur atoms, which can interact with biological targets, such as enzymes and receptors, leading to pharmacological activity.

Examples of bicyclo compounds, heterocyclic, include quinolone antibiotics (e.g., ciprofloxacin), benzodiazepines (e.g., diazepam), and camptothecin-derived topoisomerase inhibitors (e.g., irinotecan). These compounds exhibit diverse biological activities, such as antibacterial, antifungal, antiviral, anxiolytic, and anticancer properties.

Quinuclidines are a class of organic compounds that contain a unique cage-like structure consisting of a tetrahydrofuran ring fused to a piperidine ring. The name "quinuclidine" is derived from the Latin word "quinque," meaning five, and "clidis," meaning key or bar, which refers to the five-membered ring system that forms the core of these compounds.

Quinuclidines have a variety of biological activities and are used in pharmaceuticals as well as agrochemicals. Some quinuclidine derivatives have been found to exhibit anti-inflammatory, antiviral, and anticancer properties. They can also act as inhibitors of various enzymes and receptors, making them useful tools for studying biological systems and developing new drugs.

It is worth noting that quinuclidines are not typically used in medical diagnosis or treatment, but rather serve as building blocks for the development of new pharmaceutical compounds.

Tropane alkaloids are a class of naturally occurring compounds that contain a tropane ring in their chemical structure. This ring is composed of a seven-membered ring with two nitrogen atoms, one of which is part of a piperidine ring. Tropane alkaloids are found in various plants, particularly those in the Solanaceae family, which includes nightshade, belladonna, and datura. Some well-known tropane alkaloids include atropine, scopolamine, and cocaine. These compounds have diverse pharmacological activities, such as anticholinergic, local anesthetic, and central nervous system stimulant effects.

Bicyclic compounds are organic molecules that contain two rings in their structure, with at least two common atoms shared between the rings. These compounds can be found in various natural and synthetic substances, including some medications and bioactive molecules. The unique structure of bicyclic compounds can influence their chemical and physical properties, which may impact their biological activity or reactivity.

Cyclic hydrocarbons are a type of organic compounds that contain hydrogen and carbon atoms arranged in ring-like structures. These molecules are characterized by the presence of at least one closed chain of carbon atoms, forming a cycle or ring. The properties and chemical behavior of cyclic hydrocarbons depend on the number of carbon atoms in the ring, the type of bonds between them (single, double, or triple), and the presence of substituents or functional groups attached to the carbon skeleton.

Cyclic hydrocarbons can be classified into two main categories: alicyclic and aromatic compounds. Alicyclic hydrocarbons have only single bonds between the carbon atoms in their rings, while aromatic hydrocarbons contain alternating double bonds that give them unique chemical and physical properties.

Examples of cyclic hydrocarbons include cyclohexane (an alicyclic compound) and benzene (an aromatic compound). These molecules play important roles in various industrial applications, such as fuel production, pharmaceuticals, and materials science. However, some cyclic hydrocarbons can also have harmful effects on human health and the environment, making it essential to handle and dispose of them properly.

Heptanes are a group of hydrocarbons that are composed of straight-chain or branched arrangements of six carbon atoms and are commonly found in gasoline. They are colorless liquids at room temperature with a characteristic odor. In a medical context, exposure to heptanes can occur through inhalation, skin contact, or ingestion, and can cause symptoms such as headache, dizziness, nausea, and irritation of the eyes, nose, and throat. Chronic exposure has been linked to more serious health effects, including neurological damage and cancer. Proper handling and use of heptanes, as well as adequate ventilation, are important to minimize exposure and potential health risks.

Heterocyclic compounds are organic molecules that contain a ring structure made up of at least one atom that is not carbon, known as a heteroatom. These heteroatoms can include nitrogen, oxygen, sulfur, or other elements. In the case of "2-ring" heterocyclic compounds, the molecule contains two separate ring structures, each of which includes at least one heteroatom.

The term "heterocyclic compound" is used to describe a broad class of organic molecules that are found in many natural and synthetic substances. They play important roles in biology, medicine, and materials science. Heterocyclic compounds can be classified based on the number of rings they contain, as well as the types and arrangements of heteroatoms within those rings.

Two-ring heterocyclic compounds can exhibit a wide range of chemical and physical properties, depending on the nature of the rings and the heteroatoms present. Some examples of two-ring heterocyclic compounds include quinoline, isoquinoline, benzothiazole, and benzoxazole, among many others. These compounds have important applications in pharmaceuticals, dyes, pigments, and other industrial products.

Cyclooctanes are a class of organic compounds that contain a cyclic octane structure, which is an eight-carbon ring. These molecules can exist in various conformations, including "crowded" or "eclipsed" conformations, where the carbon-hydrogen bonds are arranged in a way that leads to steric strain. This strain makes cyclooctanes less stable than other cycloalkanes, such as cyclohexane. The properties and behavior of cyclooctanes can be studied and applied in fields like chemistry, biochemistry, and materials science.

Octanols are a type of chemical compound known as alcohols, specifically they are fatty alcohols with a chain of 8 carbon atoms. The most common octanol is called 1-octanol, which has the chemical formula CH3(CH2)7OH. It is a colorless oily liquid that is used in the synthesis of other chemicals and as a solvent. Octanols are often used as standards for measuring the partition coefficient between octanol and water, which is a measure of a compound's hydrophobicity or lipophilicity. This property is important in understanding how a compound may be absorbed, distributed, metabolized, and excreted in the body.

'Aza compounds' is a general term used in chemistry to describe organic compounds containing a nitrogen atom (denoted by the symbol 'N' or 'aza') that has replaced a carbon atom in a hydrocarbon structure. The term 'aza' comes from the Greek word for nitrogen, 'azote.'

In medicinal chemistry and pharmacology, aza compounds are of particular interest because the presence of the nitrogen atom can significantly affect the chemical and biological properties of the compound. For example, aza compounds may exhibit enhanced bioavailability, metabolic stability, or receptor binding affinity compared to their non-aza counterparts.

Some common examples of aza compounds in medicine include:

1. Aza-aromatic compounds: These are aromatic compounds that contain one or more nitrogen atoms in the ring structure. Examples include pyridine, quinoline, and isoquinoline derivatives, which have been used as anti-malarial, anti-inflammatory, and anti-cancer agents.
2. Aza-heterocyclic compounds: These are non-aromatic compounds that contain one or more nitrogen atoms in a cyclic structure. Examples include azepine, diazepine, and triazole derivatives, which have been used as anxiolytic, anti-viral, and anti-fungal agents.
3. Aza-peptides: These are peptide compounds that contain one or more nitrogen atoms in the backbone structure. Examples include azapeptides and azabicyclopeptides, which have been used as enzyme inhibitors and neuroprotective agents.
4. Aza-sugars: These are sugar derivatives that contain one or more nitrogen atoms in the ring structure. Examples include azasugars and iminosugars, which have been used as glycosidase inhibitors and anti-viral agents.

Overall, aza compounds represent an important class of medicinal agents with diverse chemical structures and biological activities.

The alpha7 nicotinic acetylcholine receptor (α7nAChR) is a type of cholinergic receptor found in the nervous system that is activated by the neurotransmitter acetylcholine. It is a ligand-gated ion channel that is widely distributed throughout the central and peripheral nervous systems, including in the hippocampus, cortex, thalamus, and autonomic ganglia.

The α7nAChR is composed of five subunits arranged around a central pore, and it has a high permeability to calcium ions (Ca2+). When acetylcholine binds to the receptor, it triggers a conformational change that opens the ion channel, allowing Ca2+ to flow into the cell. This influx of Ca2+ can activate various intracellular signaling pathways and have excitatory or inhibitory effects on neuronal activity, depending on the location and function of the receptor.

The α7nAChR has been implicated in a variety of physiological processes, including learning and memory, attention, sensory perception, and motor control. It has also been studied as a potential therapeutic target for various neurological and psychiatric disorders, such as Alzheimer's disease, schizophrenia, and pain.

Trypanosoma brucei rhodesiense is a species of protozoan parasite that causes African trypanosomiasis, also known as sleeping sickness, in humans. It is transmitted through the bite of an infected tsetse fly and is endemic to certain regions of East and Southern Africa.

The life cycle of T. b. rhodesiense involves two hosts: the tsetse fly and a mammalian host (such as a human). In the tsetse fly, the parasite undergoes development and multiplication in the midgut, then migrates to the salivary glands where it transforms into the metacyclic trypomastigote stage. When the infected tsetse fly bites a mammalian host, the metacyclic trypomastigotes are injected into the skin and enter the lymphatic system and bloodstream, where they multiply by binary fission as bloodstream trypomastigotes.

The symptoms of African trypanosomiasis caused by T. b. rhodesiense include fever, headache, joint pain, and itching, which may progress to more severe symptoms such as sleep disturbances, confusion, and neurological disorders if left untreated. The disease can be fatal if not diagnosed and treated promptly.

It is important to note that T. b. rhodesiense is distinct from another subspecies of Trypanosoma brucei called T. b. gambiense, which causes a different form of African trypanosomiasis that is endemic to West and Central Africa.

Stereoisomerism is a type of isomerism (structural arrangement of atoms) in which molecules have the same molecular formula and sequence of bonded atoms, but differ in the three-dimensional orientation of their atoms in space. This occurs when the molecule contains asymmetric carbon atoms or other rigid structures that prevent free rotation, leading to distinct spatial arrangements of groups of atoms around a central point. Stereoisomers can have different chemical and physical properties, such as optical activity, boiling points, and reactivities, due to differences in their shape and the way they interact with other molecules.

There are two main types of stereoisomerism: enantiomers (mirror-image isomers) and diastereomers (non-mirror-image isomers). Enantiomers are pairs of stereoisomers that are mirror images of each other, but cannot be superimposed on one another. Diastereomers, on the other hand, are non-mirror-image stereoisomers that have different physical and chemical properties.

Stereoisomerism is an important concept in chemistry and biology, as it can affect the biological activity of molecules, such as drugs and natural products. For example, some enantiomers of a drug may be active, while others are inactive or even toxic. Therefore, understanding stereoisomerism is crucial for designing and synthesizing effective and safe drugs.

Nicotinic receptors are a type of ligand-gated ion channel receptor that are activated by the neurotransmitter acetylcholine and the alkaloid nicotine. They are widely distributed throughout the nervous system and play important roles in various physiological processes, including neuronal excitability, neurotransmitter release, and cognitive functions such as learning and memory. Nicotinic receptors are composed of five subunits that form a ion channel pore, which opens to allow the flow of cations (positively charged ions) when the receptor is activated by acetylcholine or nicotine. There are several subtypes of nicotinic receptors, which differ in their subunit composition and functional properties. These receptors have been implicated in various neurological disorders, including Alzheimer's disease, Parkinson's disease, and schizophrenia.

Nicotinic agonists are substances that bind to and activate nicotinic acetylcholine receptors (nAChRs), which are ligand-gated ion channels found in the nervous system of many organisms, including humans. These receptors are activated by the endogenous neurotransmitter acetylcholine and the exogenous compound nicotine.

When a nicotinic agonist binds to the receptor, it triggers a conformational change that leads to the opening of an ion channel, allowing the influx of cations such as calcium, sodium, and potassium. This ion flux can depolarize the postsynaptic membrane and generate or modulate electrical signals in excitable tissues, such as neurons and muscles.

Nicotinic agonists have various therapeutic and recreational uses, but they can also produce harmful effects, depending on the dose, duration of exposure, and individual sensitivity. Some examples of nicotinic agonists include:

1. Nicotine: A highly addictive alkaloid found in tobacco plants, which is the prototypical nicotinic agonist. It is used in smoking cessation therapies, such as nicotine gum and patches, but it can also lead to dependence and various health issues when consumed through smoking or vaping.
2. Varenicline: A medication approved for smoking cessation that acts as a partial agonist of nAChRs. It reduces the rewarding effects of nicotine and alleviates withdrawal symptoms, helping smokers quit.
3. Rivastigmine: A cholinesterase inhibitor used to treat Alzheimer's disease and other forms of dementia. It increases the concentration of acetylcholine in the synaptic cleft, enhancing its activity at nicotinic receptors and improving cognitive function.
4. Succinylcholine: A neuromuscular blocking agent used during surgical procedures to induce paralysis and facilitate intubation. It acts as a depolarizing nicotinic agonist, causing transient muscle fasciculations followed by prolonged relaxation.
5. Curare and related compounds: Plant-derived alkaloids that act as competitive antagonists of nicotinic receptors. They are used in anesthesia to induce paralysis and facilitate mechanical ventilation during surgery.

In summary, nicotinic agonists are substances that bind to and activate nicotinic acetylcholine receptors, leading to various physiological responses. These compounds have diverse applications in medicine, from smoking cessation therapies to treatments for neurodegenerative disorders and anesthesia. However, they can also pose risks when misused or abused, as seen with nicotine addiction and the potential side effects of certain medications.

Molecular structure, in the context of biochemistry and molecular biology, refers to the arrangement and organization of atoms and chemical bonds within a molecule. It describes the three-dimensional layout of the constituent elements, including their spatial relationships, bond lengths, and angles. Understanding molecular structure is crucial for elucidating the functions and reactivities of biological macromolecules such as proteins, nucleic acids, lipids, and carbohydrates. Various experimental techniques, like X-ray crystallography, nuclear magnetic resonance (NMR) spectroscopy, and cryo-electron microscopy (cryo-EM), are employed to determine molecular structures at atomic resolution, providing valuable insights into their biological roles and potential therapeutic targets.

Molecular conformation, also known as spatial arrangement or configuration, refers to the specific three-dimensional shape and orientation of atoms that make up a molecule. It describes the precise manner in which bonds between atoms are arranged around a molecular framework, taking into account factors such as bond lengths, bond angles, and torsional angles.

Conformational isomers, or conformers, are different spatial arrangements of the same molecule that can interconvert without breaking chemical bonds. These isomers may have varying energies, stability, and reactivity, which can significantly impact a molecule's biological activity and function. Understanding molecular conformation is crucial in fields such as drug design, where small changes in conformation can lead to substantial differences in how a drug interacts with its target.

I'm sorry for any confusion, but "Pyridines" is not a medical term. It is a chemical term that refers to a class of organic compounds with the chemical structure of a six-membered ring containing one nitrogen atom and five carbon atoms (heterocyclic aromatic compound).

In a biological or medical context, pyridine derivatives can be found in various natural and synthetic substances. For example, some medications contain pyridine rings as part of their chemical structure. However, "Pyridines" itself is not a medical term or condition.

2000). "Synthesis of pharmaceutical compositions with lactams and .beta.-lactams/oxo thia azabicyclo compounds". US Patent No. ... 23 May 1985). "Method, compound and composition for effecting degradation of crude petroleum and petroleum products in an ...
... is a chemical compound. It is the base of the benzomorphan family of drugs. Benzomorphan Azocine Morphinan Ginsburg, ... David (1950). "The synthesis of morphan (2-azabicyclo[3.3.1]nonane)". Journal of Organic Chemistry. 15 (5): 1003-5. doi:10.1021 ...
This compound is then treated with one equivalent of acyl chloride to produce the stannyl monoester. Two isomers of the stannyl ... "Quaternizations in the 8-azabicyclo[4.3.0]non-3-ene series". Journal of Organic Chemistry. 39 (3): 319-321. doi:10.1021/ ... The structure of each of the two compounds contains a twisted 16-membered macrocycle. A key step in the syntheses is selective ... P. J. Crowley; M. J. T. Robinson; M. G. Ward (1977). "Conformational effects in compounds with 6-membered rings-XII". ...
... synthesis of 1-azabicyclo compounds". Chem. Commun. (16): 1168-1169. doi:10.1039/C39890001168. Hernández, R.; Medina, M.C; ... Synthesis of Chiral 7-Oxa-2-azabicyclo[2.2.1]heptane and 8-Oxa-6-azabicyclo[3.2.1]octane Ring Systems". J. Org. Chem. 68 (3): ... E. Suárez and co-workers also applied their methodology in the synthesis of chiral 8-oxa-6-azabicyclo[3.2.1]-octane 85 and 7- ... This result suggested that there is a high selectivity for the 3° hydrogen, but the intermediate tertiary chloro compound 17 is ...
They are bicyclic organic nitrogen compounds (IUPAC nomenclature: 8-methyl-8-azabicyclo[3.2.1]octane), with the chemical ... The compound is not noticeably toxic to humans. However, it stimulates specific pain receptors in the majority of mammals, ... These alkaloids cannot be substituted by any other class of compounds, so they are still in demand. This is one of the reasons ... The foliar lamina can be either simple or compound, and the latter can be either pinnatifid or ternate. The leaves have ...
... the parent compound is tropine, whose systematic name is (1R, 3r, 5S)-8-methyl-8-azabicyclo[3.2.1]octane-3-ol. In this ... More generally, iso is a compound which is isomeric to the n compound (a compound in which individual atoms or atomic groups ... for cyclo this is only the case in inorganic compounds. In organic compounds, "cyclo" is frequently used as a name component, ... Here, the compounds were designated as syn configured when the aldehyde H and the O (of the oxime) or the N (of the hydrazone) ...
Compound 7a (3′-methoxy-8-methyl-spiro(8-azabicyclo(3.2.1)octane-3,5′(4′H)-isoxazole) allosterically enhances SERT binding of ... Compounds 237a and 238a are the same compound as both are the parent for either series with a hydrogen saturated in their ... Compounds 201b & 201c were significantly more potent than cocaine while compounds 201a, 201d & 201e were significantly less ... Compounds 196k, 196n, 196o, and 197c all possess greater DAT affinity than cocaine. Compound 197b (dimethyl amide) displayed a ...
Other methods include photolysis of 2,3-diazabicyclo[2.2.1]hept-2-ene, pyrolysis of N-Phenyl-2-oxo-3-azabicyclo[2.2.1]heptane, ... The two rings are fused in a cis configuration-this meso compound formally has (1R,4S) absolute stereochemistry. The small size ...
... compound 2) (heterobivalent ligand: D2R agonist and nAChR antagonist) Oxantel α3β2-Nicotinic receptor α3β4-Nicotinic receptor ... 7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with ... "Bifunctional compounds targeting both D2 and non-α7 nACh receptors: Design, synthesis and pharmacological characterization". ... 7-azabicyclo[2.2.1]heptane 2-fluoro-3-(4-nitro-phenyl)deschloroepibatidine Coclaurine - alkaloid from Nelumbo nucifera ...
... as like upon the compounds given below. 3-Phenyl-7-azabicyclo[2.2.1]heptane derivatives Ring-contracted analogs of ... 8-azabicyclo[3.2.1]octanes and 3β-(5-Indolyl)-8-azabicyclo[3.2.1]octanes". Bioorganic & Medicinal Chemistry Letters. 11 (4): ... 3-Phenyl-9-azabicyclo[3.3.1]nonane derivatives To better elucidate the binding requirements at MAT, the methylene unit on the ... N.B. In the case of both nocaine and pethidine, N-demethyl compounds are more toxic and have a decreased seizure threshold. ...
US 5061722, Teetz, Volker; Geiger, Rolf & Urbach, Hansjorg et al., "Cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids, a ... process for their preparation, agents containing these compounds and their use", published 1991-10-29, assigned to Hoechst AG " ...
DASB compound 4b: Ki = 17 pM; 710-fold and 11,100-fold selective over DAT and NET compound (+)-12a: Ki = 180 pM at hSERT; >1000 ... Isosteres 3-cis-(3-Aminocyclopentyl)indole 8a: Ki = 220 pM allosteric modulator: 3′-Methoxy-8-methyl-spiro{8-azabicyclo[3.2.1] ... octane-3,5′(4′H)-isoxazole} (compound 7a) allosteric modulator: p-Trifluoromethyl-methcathinone The gene that encodes the ...
Compound 1d (see reference) LY-2812223 JNJ-46356479 JNJ-40411813 GSK-1331258 Imidazo[1,2-a]pyridines 3-Aryl-5-phenoxymethyl-1,3 ... 3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators". Bioorganic & Medicinal ... 5-benzodiazepin-2-one and related compounds. MNI-137 - 8-bromo-4-(2-cyanopyridin-4-yl)-1H-benzo[b][1,4]diazepin-2(3H)-one ... 2-ones 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: potent, orally stable BINA: potent; modest ago- ...
3-Quinuclidone (1-azabicyclo[2.2.2]octan-3-one) is an uneventful molecule that can be synthesized as the hydrochloric acid salt ... Quinuclidones are a class of bicyclic organic compounds with chemical formula C7H11NO with two structural isomers for the base ... This compound rapidly reacts with water to the corresponding amino acid with a chemical half-life of 15 seconds. X-ray ...
May 2008). "Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin ... November 2022). "Fractionation and Extraction Optimization of Potentially Valuable Compounds and Their Profiling in Six ... 1-azabicyclo[2.2.2]octane, and 2-(Pyridin-3-yl)-1-azabicyclo[3.2.1]octane. Anatabine Laszlo C, Kaminski K, Guan H, Fatarova M, ... made some higher potency sterically strained bicyclic analogs of anabasine: 2-(Pyridin-3-yl)-1-azabicyclo[3.2.2]nonane (TC-1698 ...
8-Azabicyclo[3.2.1]octane (tropane without the N-methyl group) is known as nortropane or nor-tropane. Phenyltropane Tropane ... Tropane is a nitrogenous bicyclic organic compound. It is mainly known for the other alkaloids derived from it, which include ... Chemical articles with multiple compound IDs, Multiple chemicals in an infobox that need indexing, Articles without KEGG source ...
Catalytic synthesis of 1-azabicyclo[4.3.0]nonanes and 1-azabicyclo[5.3.0]decanes". Khimiya Geterotsiklicheskikh Soedinenii. 6: ... Indolizidine is a heterocyclic chemical compound that forms the central core of the indolizidine alkaloids such as swainsonine ...
3. 3-Oxa-1-azabicyclo[3.3.1]nonan-2-one and 6-oxa-1-azabicyclo[3.2.1]octan-7-one, two atom-bridged bicyclic urethanes ... There has been an active research program to seek compounds inconsistent with the rule, and for bicyclic systems a limit of S ... Köbrich, Gert (1973). "Bredt Compounds and the Bredt Rule". Angew. Chem. Int. Ed. 12 (6): 464-473. doi:10.1002/anie.197304641. ... but the similar compound bicyclo[2.2.1]heptan-7-one-1-carboxylic acid remains stable beyond 500 °C, despite both being β-keto ...
The Blum-Ittah aziridine synthesis has been used in the synthesis of α-methylserine and 6-Azabicyclo[3.2.1]octanes. Hassner, ... Biologically Active Compounds Based on Renewable Raw Materials". European Journal of Organic Chemistry. 2003 (4): 649-659. doi: ... Pulipaka, Aravinda B.; Bergmeier, Stephen C. (2008-01-23). "A Synthesis of 6-Azabicyclo[3.2.1]octanes. The Role of N- ...
The first step includes a reaction between a compound containing acidic C-H hydrogens, an aldehyde and a primary amine, using a ... Jeyaraman, R.; Avila, S. (1981). "Chemistry of 3-Azabicyclo[3.3.1]nonanes". Chemical Reviews. 81 (2): 149-174. doi:10.1021/ ... Bispidine (3,7-diazabicyclo[3.3.1]nonane) is an organic compound that is classified as a bicyclic diamine. Although synthetic, ... compounds with tetradentate ligands based on the bispidine backbone". Journal of the Chemical Society, Dalton Transactions (23 ...
July 2010). "6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple ... WO 2008031772, Bertani, Barbara; Di Fabio, Romano & Micheli, Fabrizio et al., "Azabicyclic compounds as inhibitors of ...
The structurally related compound (-)-2β-(3-methyl-5-isoxazolyl)nortropane is a potent and selective agonist for nicotinic ... and 3-isoxazolyl-8-azabicyclo[3.2.1]octanes". Bioorganic & Medicinal Chemistry Letters. 14 (7): 1775-8. doi:10.1016/j.bmcl. ...
If the exo ethyl group on the 2-azabicyclo[2.2.2]octane system in ibogaine is replaced with an endo ethyl, then epiibogaine is ... Ibogaine and related indole compounds are susceptible to oxidation over time. The National Institute on Drug Abuse (NIDA) began ... Then, using 7-ethyl-2-azabicyclo[2.2.2]oct-5-ene and cesium carbonate in acetonitrile, the ibogaine precursor 7-ethyl-2-(2-(2- ... Ibogaine: A Novel Anti-Addictive Compound - A Comprehensive Literature Review Jonathan Freedlander, University of Maryland ...
Synthesis of aza-bicyclo[3.2.1]octane and aza-bicyclo[3.2.2]nonane ethers, imides, and amines". The Journal of Organic ... NS2214 appears to have been abandoned now, RTI-336 was their latest compound. RTI decided that they wanted to make all 8 ... To solve the problem of the unexpected aza-bicyclo[3.2.2]nonane rearrangement product, the original synthesis had to be ... and ligand binding of tropane ring analogs of paroxetine and an unexpected aza-bicyclo[3.2.2]nonane rearrangement product". ...
Carreras J, Avenoza A, Busto JH, Peregrina JM (April 2007). "Synthesis of azabicyclo[2.2.n]alkane systems as analogues of 3-[1- ... 3-Pyridyl compounds, Pyrrolidines, Stimulants, All stub articles, Nervous system drug stubs). ... is widely used in scientific research into the structure and function of this receptor subtype and has been the lead compound ...
May 2008). "Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin ... It has neuroprotective effects in animal studies, and has been used as a lead compound to find further potent derivatives. ... Marrero MB, Papke RL, Bhatti BS, Shaw S, Bencherif M (April 2004). "The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[ ... yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands". The Journal of Organic Chemistry. ...
Heesing, A.; Herdering, W. (January 1981). "Sauerstoff-insertion bei der umlagerung von 2-aza-bicyclo[2.2.1]hept-2-enderivaten ... X/1, 4th Edition: Nitro, Nitroso and Hydroxylamine Compounds (4 ed.). Georg Thieme Verlag. p. 1266. ISBN 9783131805546. Ayres, ... Application to the synthesis of heterocyclic compounds". Journal of Heterocyclic Chemistry. 33 (5): 1489-1496. doi:10.1002/jhet ...
Reed, D. D.; Bergmeier, S. C. (2007). "A Facile Synthesis of a Polyhydroxylated 2-Azabicyclo[3.2.1]octane". J. Org. Chem. 72 (3 ... Meier, H.; Zeller, K.-P. (1975). "The Wolff Rearrangement of α-Diazo Carbonyl Compounds". Angew. Chem. Int. Ed. 14 (1): 32-43. ... Ye, T.; McKervey, M. A. (1994). "Organic Synthesis with α-Diazo Carbonyl Compounds". Chem. Rev. 94 (4): 1091-1160. doi:10.1021/ ...
Slow addition of the hydrazone is not necessary and it was found that this procedure is better suited for carbonyl compounds ... Bosch, J.; Bonjoch, J. (1981). "Synthetic route to 6-functionalized 2-azabicyclo\3.3.1]nonanes". The Journal of Organic ... Several of the presented procedures require isolation of the hydrazone compound prior to reduction. This can be complicated by ... The reactions of hydrazones and related compounds with strong bases. Part I. A modified Wolff?Kishner procedure". Journal of ...
A lactim is a cyclic imidic acid compound characterized by an endocyclic carbon-nitrogen double bond. They are formed when ... 2012, 112 (8), pp 4642-4686."2-Azabicyclo[2.2.1]hept-5-en-3-one: Chemical Profile of a Versatile Synthetic Building Block and ...
2000). "Synthesis of pharmaceutical compositions with lactams and .beta.-lactams/oxo thia azabicyclo compounds". US Patent No. ... 23 May 1985). "Method, compound and composition for effecting degradation of crude petroleum and petroleum products in an ...
Compound overview, Drug targets, Compound forms, Similar compounds , canSARS ... Compound 3-(4-Fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester , 3-(4-Fluoro-phenyl)-8-methyl- ... 3-(4-Fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester ...
DIFLUORO-SUBSTITUTED AZABICYCLO COMPOUNDS AND USES THEREOF. Disclosed are a series of difluoro-substituted azabicyclo compounds ... COMPOUND AS CDK7 KINASE INHIBITOR AND USE THEREOF. A compound as a CDK7 kinase inhibitor and the use thereof. The compound has ... COMPOUND USED AS WDR5 INHIBITOR OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND USE OF COMPOUND. Provided are a compound used ... The present compounds may be useful as ... WO/2024/014885A1 NOVEL BICYCLIC HETEROARYL COMPOUND AND USE THEREOF. The present ...
... review offers a systematic analysis of literature data about intramolecular C-H insertion reactions of diazocarbonyl compounds ... The change of catalyst allowed to obtain the target 3-oxa-1-azabicyclo[4.2.0]octane 11 in 47% yield, followed by standard ... 11 The insertion of diazo compounds at the C-H bond in the synthesis of heterocyclic compounds was developed by Davies,12 , 13 ... The bicyclic compound 60 was further transformed to dihydroxylated compound 61 by the transformation of the tetrahydrofuranone ...
The chemical name is (5R,6S)-3-[[2-(formimidoylamino)ethyl]thio]-6-[(R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2- ... It is an off-white to white, hygroscopic, amorphous compound, very soluble in water. The empirical formula is C16H25N2NaO5S and ... It is an off-white, nonhygroscopic crystalline compound, sparingly soluble in water. The empirical formula is C12H17N3O4S.H2O ...
150000001875 compounds Chemical class 0.000 claims description 5 * 102000035195 Peptidases Human genes 0.000 claims description ... JGSARLDLIJGVTE-UHFFFAOYSA-N 3,3-dimethyl-7-oxo-6-[(2-phenylacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid ... RASZIXQTZOARSV-BDPUVYQTSA-N astacin Chemical compound CC=1C(=O)C(=O)CC(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C= ... MQZIGYBFDRPAKN-ZWAPEEGVSA-N astaxanthin Chemical compound C([C@H](O)C(=O)C=1C)C(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC ...
1R,2R,4S)-2-(6-Chloropyridin-3-yl)-2-methyl-7-azabicyclo[2.2.1]heptane. 222.71 C12H15ClN2. ... Plant Compounds. Floral Compounds. Semiochemicals & Taxa. Synthesis. ID Tools. Control. Invasive spp.. References. Abstract. ... 1R,2R,4S)-2-(6-Chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane. 208.69 C11H13ClN2. ...
The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention ... The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically ... The compound of claim 1, wherein said compound is 3-(6-methyl-pyrimidin-4-yl)-3-aza-bicyclo[3.2.1]oct-8-yl-[8-(2,3,4-trifluoro- ... The title compound was prepared in analogy to example 24f from (rac)-9-endo/exo-3-oxa-7-aza-bicyclo[3.3.1]non-9-yl)-[8-(2,3,4- ...
Renal excretion of unchanged compound was negligible across species. Similarly, unchanged compound excreted in the bile was ... PF-06835919 [(1R,5S,6R)-3-(2-[(2S)-2-Methylazetidin-1-yl]-6-(trifluoromethyl)pyrimidin-4-yl)3-azabicyclo[3.1.0]hex-6-yl]acetic ... nonlabeled compounds). Intracellular accumulation for radiolabeled compounds was determined either by mixing the cell lysate ... At this time point, the compound is approaching terminal phase after intravenous dosing (Supplemental Fig. 3), and therefore ...
2R-(2α,3Z,5α)]-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, compound with tert-butylamine ...
Azabicyclo Compounds. *Bile Ducts. *Biliary Tract Neoplasms. *Biomedical Research. *Body Image. *Boston ...
Gliclazide is 1-(3-azabicyclo[3.3.0]oct-3-yl)-3-(p-tolylsulfonyl)urea. It differs from other related compounds by the addition ...
... for price inquiry.where to buy 4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylicacid, 6-[[(2R)-2-carboxy-2-(3-thienyl)acetyl]amino ... 3,3-dimethyl-7-oxo-, sodiumsalt (1:2), (2S,5R,6R)-.Also offer free database of 4-Thia-1-azabicyclo[3.2.0]heptane-2- ... Find quality suppliers and manufacturers of 4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylicacid, 6-[[(2R)-2-carboxy-2-(3-thienyl ... 4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylicacid, 6-[[(2R)-2-carboxy-2-(3-thienyl)acetyl]amino]-3,3-dimethyl-7-oxo-, ...
3-Azabicyclo[3.1.0]hexanes are common structural components in natural products and bioactive compounds. Traditionally, the ... This reaction was tailor-made for saturated aza[3.1.0] bicycle-containing fused bicyclic compounds that may be applied in the ...
Pre incubation of enzyme with compounds was carried out by exposing the enzyme to compounds before addition of the substrate ... The substitution pattern about the azabicyclo octane and azabicyclo nonane ring methods influences five HT three binding ... Test compounds had been given orally 1 h prior to restraint tension, five HT or TRH. Stool excretion was observed for one h ... Despite constrained publicly on the market VEGFR Inhibitor details within the compound and its use, Celgene has stated that CC ...
5 x V37: [(1R,5S)-8-PHENETHYL-8-AZABICYCLO[3.2.1]OCTAN-3-YL] BENZOATE(Non-covalent). V37.1: 15 residues within 4Å:*. Chain A: T ... Compound 4) Coordinates. PDB Format Method. X-RAY DIFFRACTION 3.30 Å. Oligo State. homo-pentamer. Ligands ...
With reactant compound containing at least two -C-C(=X)-X-C groups and which compound is devoid of C-NH, C=NH or C-N(H)-H ... 1-thia-5-aza-bicyclo (4.2.0) octane ring containing (including dehydrogenated) (e.g., cephalosporins, etc.) : Additional hetero ... With reactant compound containing at least two -C-C(=X)-X-C groups and which compound is devoid of C-NH, C=NH or C-N(H)-H ... ORGANIC COMPOUNDS -- PART OF THE CLASS 532-570 SERIES : : Carboxylic acid anhydrides (i.e., compounds having the -C(=O)-O-C(=O ...
It becomes a choice of lead compound for new researchers due to its wide variety of pharmacological activities and so on. We ... and 8-Azabicyclo[5.1.0]octane (22.035%). Hence, the inhibitory effects of bitter cola leaf on Cucumber fruit rot fungal ... The predominant compounds include 2,5-Methanofuro[3,2-b]pyridine, octahydro- (21.416%), 5-Amino-2-methoxy phenol (17.539%), 2,5 ... The Gas Chromatography-Mass Spectrometry (GC-MS) analysis, revealed the presence of 30 bioactive compounds with a variety of ...
Nowadays the necessity to design new compounds to overcome this resistance has Libraries become one of the most important areas ... 4-diaryl-3-azabicyclo[3.3.1]nonane-9-one-O-[2,4,6-tritertiarybutylcyclohexa-2,5-dienon-4-yl]oximes [9-12]. The aim of this work ... The structure of the synthesized compounds [9-12] is discussed with the help of melting points, elemental analysis, FT-IR, MS, ... Results Chemical Analysis One known compound: 3-O-β-D-glucopyranoside of sitosterol (1), and a mixture of β-sitosterol, ...
The IUPAC name for 7-ADD is (6R,7R)-7-amino-8-oxo-3-(prop-2-en-1-yl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, and ... This compound is ideal for researchers studying the effects of synthetic cannabinoids on the brain and behavior due to its ... CBD Powder for sale CBD Powder is a pure and potent form of cannabidiol, one of the many naturally occurring compounds found in ... The IUPAC name for 7-ABF is (7-azabenzofuran-5-yl)boronic acid, and its CAS number is 929900-57-1. This compound is highly ...
Azabicyclo Compounds D4.75.80.875.99 D3.605.84.500 Azacosterol D4.808.247.222.284.70 D4.210.500.247.222.284.70 D4.808.247.808. ... Heterocyclic Compounds with 4 or More Rings D3.549 D3.633.400 (Replaced for 2016 by Heterocyclic Compounds, 4 or More Rings) ... Bicyclo Compounds, Heterocyclic D2.455.426.100.80.85 D3.438.260 D4.75.80.875 (Replaced for 2016 by Bridged Bicyclo Compounds, ... Heterocyclic Compounds, 2-Ring D3.438 D3.633.100 Heterocyclic Compounds, 3-Ring D3.494 D3.633.300 Heterotrophic Processes ...
Azabicyclo Compounds D4.75.80.875.99 D3.605.84.500 Azacosterol D4.808.247.222.284.70 D4.210.500.247.222.284.70 D4.808.247.808. ... Heterocyclic Compounds with 4 or More Rings D3.549 D3.633.400 (Replaced for 2016 by Heterocyclic Compounds, 4 or More Rings) ... Bicyclo Compounds, Heterocyclic D2.455.426.100.80.85 D3.438.260 D4.75.80.875 (Replaced for 2016 by Bridged Bicyclo Compounds, ... Heterocyclic Compounds, 2-Ring D3.438 D3.633.100 Heterocyclic Compounds, 3-Ring D3.494 D3.633.300 Heterotrophic Processes ...
The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds ... 2S,3R)-N-2-3-PYRIDINYLMETHYL-1-AZABICYCLO 2.2.2 OCT-3-YL BENZOFURAN-2-CARBOXAMIDE, NOVEL SALT FORMS, AND METHODS OF USE THEREOF ... The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds ... The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds ...
Bulk for Human Drug Compounding, and Bulk for Animal Drug Compounding. FDA does not review and approve unfinished products. ... Ramipril, USP is a 2‑aza‑bicyclo [3.3.0]‑octane‑3‑carboxylic acid derivative. It is a white to almost white, crystalline powder ...
8-Azabicyclo[3.2.1]octan-8-ol (ABOOL) and 7-azabicyclo[2.2.1]heptan-7-ol (ABHOL) feature small bicyclic backbones and are known ... Oxidation of Alcohols to Carbonyl Compounds with Diisopropyl Azodicarboxylate Catalyzed by Nitroxyl Radicals ...
Heterocyclic Compounds, 2-Ring [D03.438]. *Purines [D03.438.759]. *Purinones [D03.438.759.758]. *Hypoxanthines [D03.438.759.758 ...
Azabicyclo Compounds. Compuestos de Azabiciclo. Cucurbitacinas. Cucurbitacins. Cucurbitacinas. Fenamatos. Fenamates. Fenamatos ...
Heterocyclic Compounds [D03] * Heterocyclic Compounds, Fused-Ring [D03.633] * Heterocyclic Compounds, 2-Ring [D03.633.100] * ... 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((hydroxyphenylacetyl)amino)-3-(((1-methyl-1H-tetrazol-5-yl)thio) ... Compound 83405 Narrower Concept UI. M0354276. Registry Number. 0. Terms. Compound 83405 Preferred Term Term UI T007071. Date07/ ... Sulfur Compounds [D02.886] * Thiazines [D02.886.665] * Cephalosporins [D02.886.665.074] * Cefamandole [D02.886.665.074.150] * ...
IUPAC Name: [(3S,7S)-7-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2R)-3-hydroxy-2-phenylpropanoate , CAS Registry Number: ... Synonyms: p-Anisil, 4,4-Dimethoxybenzil, Di-p-anisoyl, p,p-Dimethoxybenzil, Benzil-based compound, 21, Bis(4-methoxyphenyl) ...
7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid (82768-37-4) ... Related compounds:. *Nitriles. See other substances:. *6-methylcarbostyril (4053-34-3). *4-chloro-2-(methylsulfanyl-methyl)- ... 3-nitrobenzyl 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate ...
  • It was shown that the protective group at nitrogen atom must be unreactive towards metallocarbenoids, while also promoting intramolecular insertion at C-H bonds, forming nitrogen-containing heterocyclic compounds. (springer.com)
  • This has been shown both by genetic means, i.e., ablation of the presenilin genes and by low-molecular-weight inhibitory compounds. (justia.com)
  • It is therefore of interest to develop novel compounds, which act as ligands for the o7 nAChR subtype, for the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors. (allindianpatents.com)
  • This invention relates to novel compounds, which act as ligands for the a7 nAChR subtype, methods of preparing such compounds, compositions comprising such compounds, and methods of use thereof. (allindianpatents.com)
  • Provided herein are novel compounds, e.g., those of Formula (I), as GCN2 inhibitors. (sumobrain.com)
  • Also provided are pharmaceutical compositions including one or more of the novel compounds, and pharmaceutical uses thereof. (sumobrain.com)
  • This review is dedicated to carbenoid reactions at С-Н bonds as key steps in the total synthesis of some natural compounds and their synthetic analogs, characterized by a broad range of biological activity. (springer.com)
  • Such C-H insertion reactions are the key steps in many syntheses of heterocyclic systems, analogs of natural compounds. (springer.com)
  • This study aimed to evaluate CL medium in comparison with CSL one for detecting the natural compounds produced from R. oryzae . (vetmedmosul.com)
  • It is designated chemically as 8-azabicyclo[3.2.1] octane, 3-(diphenylmethoxy)-, endo , methanesulfonate. (nih.gov)
  • It differs from other related compounds by the addition of an aza-bicyclo octane ring. (rosepharmacy.com)
  • The present invention provides a novel compound represented by chemical formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof. (sumobrain.com)
  • The application relates to vinyl thianthrenium compounds Vinyl- TT+X- of the Formula (I), a process for preparing the same and the use thereof for vinylating organic compounds. (sumobrain.com)
  • The present application provides a compound represented by formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same. (sumobrain.com)
  • Specifically, the present invention relates to a pharmaceutical combination of a compound of formula I, a tautomer thereof or a pharmaceutically acceptable salt thereof, and az. (sumobrain.com)
  • Disclosed are a series of difluoro-substituted azabicyclo compounds and uses thereof, and specifically disclosed are a compound represented by formula (V) and a pharmaceutically acceptable salt thereof. (sumobrain.com)
  • Provided are a deuterated compound represented by formula IA or a pharmaceutically acceptable salt thereof, a preparation method therefor and a use thereof. (sumobrain.com)
  • It is an off-white, nonhygroscopic crystalline compound, sparingly soluble in water. (globalrph.com)
  • A yellow, crystalline solid compound. (medindex.am)
  • Gliclazide is 1-(3-azabicyclo[3.3.0]oct-3-yl)-3-(p-tolylsulfonyl)urea. (rosepharmacy.com)
  • Benztropine mesylate is a synthetic compound containing structural features found in atropine and diphenhydramine. (nih.gov)
  • GC-MA analysis appeared several different compounds in the crude extracts of R. oryzae using these fermenting synthetic media; however, some compounds were reported to be similar in their structures. (vetmedmosul.com)
  • The chemistry of diazo compounds has a long history, including the frequent application of these reactants in organic synthesis, for example, as carbene and carbenoid precursors. (springer.com)
  • Compounds represented by general formula (1), the compounds having strong inhibitory action against mPGES-1 and being useful as active ingredients for pharmaceuticals for the treatment of inflammation and the like. (sumobrain.com)
  • The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome. (justia.com)
  • Diazo compounds can be easily prepared by convenient procedures and possess various reactivity, depending on the structure. (springer.com)
  • Provided herein are methods of preparation of compound 101. (sumobrain.com)
  • Also provided are intermediate compounds useful in the preparation of compound 101, and methods of preparation of those intermediate compounds. (sumobrain.com)
  • An efficient one-pot amination/lactamisation sequence for the preparation of 2-azabicyclo[2.2.2]octanones from 6-carboalkoxycyclohex-2-enones and aqueous ammonia is described. (york.ac.uk)
  • In industrial mycology, the fungus was tested to activate antioxidant compounds in the food preparation such as the cake of pumpkin oil (14). (vetmedmosul.com)
  • This review offers a systematic analysis of literature data about intramolecular C-H insertion reactions of diazocarbonyl compounds, applicable to the synthesis of biologically active nitrogen- and oxygen-containing heterocyclic systems. (springer.com)
  • Scope and limitation studies are reported for this tandem procedure and a range of bicyclic compounds have been prepared, two of which were characterised by X-ray crystallography. (york.ac.uk)
  • It is an off-white to white, hygroscopic, amorphous compound, very soluble in water. (globalrph.com)
  • With an excellent inhibitory activity against PIKfyve, the novel compound of the. (sumobrain.com)
  • Compounds which show this effect on modulating γ-secretase activity include certain non-steroidal anti-inflammatory drugs (NSAIDs) and related analogues (Weggen et al. (justia.com)
  • Some of compounds exhibited significant anti-inflammatory activities in vitro via suppressing the production of pro-inflammatory cytokine IL-1ß. (bvsalud.org)
  • Notably, compound 4, the most active enantiomeric pair in vitro, displayed prominent potent protecting activity against liver injury at a low dose of 3 mg/kg in mice, which could serve as a promising lead for the development of acute liver injury therapeutic agent. (bvsalud.org)
  • Since natural products have multiple targets and often are multifunctional, making them promising compounds for the treatment of diabetes, we identified Drak2 inhibitors from a natural product library. (bvsalud.org)
  • Benztropine mesylate is a synthetic compound containing structural features found in atropine and diphenhydramine. (nih.gov)
  • Among the identified products, luteolin, a flavonoid, was found to be the most effective compound. (bvsalud.org)
  • Thirty-three percent to 67% of a ceftriaxone dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds. (nih.gov)
  • One VMG program is the rodent Hershberger bioassay, which is intended to be used as a screen for suspected androgen agonists and antagonists, and to assist in compound prioritization for further evaluation. (nih.gov)
  • A new class of potent liver injury protective compounds, phychetins A-D (1-4) featuring an unique 6/6/5/6/5 pentacyclic framework, were isolated and structurally characterized from a Chinese medicinal plant Phyllanthus franchetianus. (bvsalud.org)