Tetrazoles are heterocyclic organic compounds containing a 1,3,5-triazole ring with an additional nitrogen atom, often used in pharmaceuticals as bioisosteres for carboxylic acid groups due to their isoelectronic nature and similar hydrogen bonding capabilities.
Water swollen, rigid, 3-dimensional network of cross-linked, hydrophilic macromolecules, 20-95% water. They are used in paints, printing inks, foodstuffs, pharmaceuticals, and cosmetics. (Grant & Hackh's Chemical Dictionary, 5th ed)
Organic chemistry methodology that mimics the modular nature of various biosynthetic processes. It uses highly reliable and selective reactions designed to "click" i.e., rapidly join small modular units together in high yield, without offensive byproducts. In combination with COMBINATORIAL CHEMISTRY TECHNIQUES, it is used for the synthesis of new compounds and combinatorial libraries.
Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)
Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS.
That portion of the electromagnetic spectrum immediately below the visible range and extending into the x-ray frequencies. The longer wavelengths (near-UV or biotic or vital rays) are necessary for the endogenous synthesis of vitamin D and are also called antirachitic rays; the shorter, ionizing wavelengths (far-UV or abiotic or extravital rays) are viricidal, bactericidal, mutagenic, and carcinogenic and are used as disinfectants.
Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.
Acrylic acids or acrylates which are substituted in the C-2 position with a methyl group.

Irbesartan reduces QT dispersion in hypertensive individuals. (1/2330)

Angiotensin type 1 receptor antagonists have direct effects on the autonomic nervous system and myocardium. Because of this, we hypothesized that irbesartan would reduce QT dispersion to a greater degree than amlodipine, a highly selective vasodilator. To test this, we gathered electrocardiographic (ECG) data from a multinational, multicenter, randomized, double-blind parallel group study that compared the antihypertensive efficacy of irbesartan and amlodipine in elderly subjects with mild to moderate hypertension. Subjects were treated for 6 months with either drug. Hydrochlorothiazide and atenolol were added after 12 weeks if blood pressure (BP) remained uncontrolled. ECGs were obtained before randomization and at 6 months. A total of 188 subjects (118 with baseline ECGs) were randomized. We analyzed 104 subjects who had complete ECGs at baseline and after 6 months of treatment. Baseline characteristics between treatments were similar, apart from a slight imbalance in diastolic BP (irbesartan [n=53] versus amlodipine [n=51], 99.2 [SD 3. 6] versus 100.8 [3.8] mm Hg; P=0.03). There were no significant differences in BP normalization (diastolic BP <90 mm Hg) between treatments at 6 months (irbesartan versus amlodipine, 80% versus 88%; P=0.378). We found a significant reduction in QT indexes in the irbesartan group (QTc dispersion mean, -11.4 [34.5] milliseconds, P=0.02; QTc max, -12.8 [35.5] milliseconds, P=0.01), and QTc dispersion did not correlate with the change in BP. The reduction in QT indexes with amlodipine (QTc dispersion, -9.7 [35.4] milliseconds, P=0.06; QTc max, -8.6 [33.2] milliseconds, P=0.07) did not quite reach statistical significance, but there was a correlation between the change in QT indexes and changes in systolic BP. In conclusion, irbesartan improved QT dispersion, and this effect may be important in preventing sudden cardiac death in at-risk hypertensive subjects.  (+info)

Blocking angiotensin II ameliorates proteinuria and glomerular lesions in progressive mesangioproliferative glomerulonephritis. (2/2330)

BACKGROUND: The renin-angiotensin system is thought to be involved in the progression of glomerulonephritis (GN) into end-stage renal failure (ESRF) because of the observed renoprotective effects of angiotensin-converting enzyme inhibitors (ACEIs). However, ACEIs have pharmacological effects other than ACE inhibition that may help lower blood pressure and preserve glomerular structure. We previously reported a new animal model of progressive glomerulosclerosis induced by a single intravenous injection of an anti-Thy-1 monoclonal antibody, MoAb 1-22-3, in uninephrectomized rats. Using this new model of progressive GN, we examined the hypothesis that ACEIs prevent the progression to ESRF by modulating the effects of angiotensin II (Ang II) on the production of transforming growth factor-beta (TGF-beta) and extracellular matrix components. METHODS: We studied the effect of an ACEI (cilazapril) and an Ang II type 1 receptor antagonist (candesartan) on the clinical features and morphological lesions in the rat model previously reported. After 10 weeks of treatment with equihypotensive doses of cilazapril, cilazapril plus Hoe 140 (a bradykinin receptor B2 antagonist), candesartan, and hydralazine, we examined systolic blood pressure, urinary protein excretion, creatinine clearance, the glomerulosclerosis index, and the tubulointerstitial lesion index. We performed a semiquantitative evaluation of glomerular immunostaining for TGF-beta and collagen types I and III by immunofluorescence study and of these cortical mRNA levels by Northern blot analysis. RESULTS: Untreated rats developed massive proteinuria, renal dysfunction, and severe glomerular and tubulointerstitial injury, whereas uninephrectomized control rats did not. There was a significant increase in the levels of glomerular protein and cortical mRNA for TGF-beta and collagen types I and III in untreated rats. Cilazapril and candesartan prevented massive proteinuria, increased creatinine clearance, and ameliorated glomerular and tubulointerstitial injury. These drugs also reduced levels of glomerular protein and cortical mRNA for TGF-beta and collagen types I and III. Hoe 140 failed to blunt the renoprotective effect of cilazapril. Hydralazine did not exhibit a renoprotective effect. CONCLUSION: These results indicate that ACEIs prevent the progression to ESRF by modulating the effects of Ang II via Ang II type 1 receptor on the production of TGF-beta and collagen types I and III, as well as on intrarenal hemodynamics, but not by either increasing bradykinin activity or reducing blood pressure in this rat model of mesangial proliferative GN.  (+info)

Resetting of exaggerated tubuloglomerular feedback activity in acutely volume-expanded young SHR. (3/2330)

One purpose of the present study was to evaluate the ability of 7-wk-old spontaneously hypertensive rats (SHR) to reset tubuloglomerular feedback (TGF) activity in response to acute volume expansion (VE). Second, we evaluated the contribution of ANG II, via its action on AT1 receptors, to TGF control of glomerular function during VE. TGF was assessed by micropuncture methods and proximal tubular stop-flow pressure (SFP) determinations in SHR, Wistar-Kyoto rats (WKY), and Sprague-Dawley rats (SD). During euvolemia SHR exhibited enhanced TGF activity. In the same animals acute VE was achieved by infusion of saline (5 ml. h-1. 100 g body wt-1). VE led to resetting of TGF in all three strains. Maximal SFP responses, elicited by a 30-40 nl/min loop of Henle perfusion rate, decreased from 19 to 12 mmHg in SHR and, on average, from 11 to 5 mmHg in WKY and SD (P < 0.001). Tubular flow rate producing a half-maximal response (turning point) shifted to higher flow rates during VE, from 12 to 14 nl/min in SHR and from 15 to 19 nl/min in WKY. Administration of the AT1 receptor blocker candesartan (0.05 mg/kg iv) during sustained VE decreased TGF-mediated reductions in SFP in SHR and slightly increased the turning point in WKY. Nevertheless, other parameters of TGF activity were unaffected by AT1 receptor blockade. In conclusion, young SHR possess the ability to reset TGF activity in response to VE to a degree similar to compensatory adjustments in WKY. However, TGF remains enhanced in SHR during VE. ANG II and its action on AT1 receptors are in part responsible for the exaggerated SFP responses in young SHR during VE.  (+info)

ACE inhibition and ANG II receptor blockade improve glomerular size-selectivity in IgA nephropathy. (4/2330)

Protein trafficking across the glomerular capillary has a pathogenic role in subsequent renal damage. Despite evidence that angiotensin-converting enzyme (ACE) inhibitors improve glomerular size-selectivity, whether this effect is solely due to ANG II blocking or if other mediators also play a contributory role is not clear yet. We studied 20 proteinuric patients with IgA nephropathy, who received either enalapril (20 mg/day) or the ANG II receptor blocker irbesartan (100 mg/day) for 28 days in a randomized double-blind study. Measurements of blood pressure, renal hemodynamics, and fractional clearance of neutral dextran of graded sizes were performed before and after 28 days of treatment. Both enalapril and irbesartan significantly reduced blood pressure over baseline. This reduction reached the maximum effect 4-6 h after drug administration but did not last for the entire 24-h period. Despite transient antihypertensive effect, proteinuria was effectively reduced by both treatments to comparable extents. Neither enalapril nor irbesartan modified the sieving coefficients of small dextran molecules, but both effectively reduced transglomerular passage of large test macromolecules. Theoretical analysis of sieving coefficients showed that neither drug affected significantly the mean pore radius or the spread of the pore-size distribution, but both importantly and comparably reduced the importance of a nonselective shunt pathway. These data suggest that antagonism of ANG II is the key mechanism by which ACE inhibitors exert their beneficial effect on glomerular size-selective function and consequently on glomerular filtration and urinary output of plasma proteins.  (+info)

Angiotensin II receptor blockade in normotensive subjects: A direct comparison of three AT1 receptor antagonists. (5/2330)

Use of angiotensin (Ang) II AT1 receptor antagonists for treatment of hypertension is rapidly increasing, yet direct comparisons of the relative efficacy of antagonists to block the renin-angiotensin system in humans are lacking. In this study, the Ang II receptor blockade induced by the recommended starting dose of 3 antagonists was evaluated in normotensive subjects in a double-blind, placebo-controlled, randomized, 4-way crossover study. At 1-week intervals, 12 subjects received a single dose of losartan (50 mg), valsartan (80 mg), irbesartan (150 mg), or placebo. Blockade of the renin-angiotensin system was assessed before and 4, 24, and 30 hours after drug intake by 3 independent methods: inhibition of the blood pressure response to exogenous Ang II, in vitro Ang II receptor assay, and reactive changes in plasma Ang II levels. At 4 hours, losartan blocked 43% of the Ang II-induced systolic blood pressure increase; valsartan, 51%; and irbesartan, 88% (P<0.01 between drugs). The effect of each drug declined with time. At 24 hours, a residual effect was found with all 3 drugs, but at 30 hours, only irbesartan induced a marked, significant blockade versus placebo. Similar results were obtained when Ang II receptor blockade was assessed with an in vitro receptor assay and by the reactive rise in plasma Ang II levels. This study thus demonstrates that the first administration of the recommended starting dose of irbesartan induces a greater and longer lasting Ang II receptor blockade than that of valsartan and losartan in normotensive subjects.  (+info)

Effects of BAY 10-6734 (Embusartan), a new angiotensin II type I receptor antagonist, on vascular smooth muscle cell growth. (6/2330)

Angiotensin II (AII), an important hypertrophic factor in the cardiovascular system, exerts most of its known effects in vivo through the AII receptor type 1 (AT1) subclass of AII receptors. These receptors are also responsible for the growth-related effects of AII in cultured vascular smooth muscle cells (VSMCs). We presently investigated the effects of BAY 10-6734 (Embusartan), a new orally active AT1 antagonist, on VSMC growth and proliferation of cultured VSMCs isolated from the aortae of Wistar Kyoto rats and spontaneously hypertensive rats. BAY 10-6734 and losartan (considered as AT1 receptor antagonist of reference), as well as their respective active metabolites, were studied for their inhibition of: 1) [125I]AII binding to its receptors, 2) AII-induced DNA and protein synthesis (by measuring the incorporation of 5-bromo-2'-deoxyuridine and [3H]L-leucine, respectively), and 3) AII-induced variations in intracellular Ca2+ concentration, using cells labeled with Fura-2. All of the tested compounds inhibited the aforementioned parameters in a concentration-dependent manner. Half-maximal inhibitory concentration values indicated that BAY 10-6734 was significantly more potent than losartan and that spontaneously hypertensive rat-derived VSMCs were more sensitive than Wistar Kyoto rat-derived ones. Neither BAY 10-6734 nor losartan affected the intracellular Ca2+ concentration of unstimulated VSMCs but both compounds inhibited both AII-induced Ca2+ mobilization from internal stores and Ca2+ influx. Neither compound affected arginine-vasopressin-, basic fibroblast growth factor-, or serum-induced DNA and protein synthesis. BAY 10-6734 appears therefore as a potent and specific new inhibitor of AII-induced growth-related events in VSMCs.  (+info)

Serial changes in sarcoplasmic reticulum gene expression in volume-overloaded cardiac hypertrophy in the rat: effect of an angiotensin II receptor antagonist. (7/2330)

This study was designed to clarify whether gene expression in the cardiac sarcoplasmic reticulum [sarcoplasmic reticulum Ca2+-ATPase (SERCA), phospholamban, ryanodine receptor and calsequestrin] changes in accordance with left ventricular functional alterations in the volume-overloaded heart. Further, the effect of the angiotensin II type 1 receptor antagonist, TCV-116, on the expression of these genes was also evaluated. Left ventricular fractional shortening was significantly increased at 7 days, had returned to control levels at 21 days, and had significantly decreased at 35 days after the shunt operation, compared with sham-operated rats. The level of SERCA mRNA was significantly decreased at both 21 days and 35 days after the shunt operation. The levels of ryanodine receptor and phospholamban mRNAs were significantly decreased at 35 days in shunt-operated rats. The decrease in the SERCA mRNA level preceded the development of cardiac dysfunction. The levels of SERCA and ryanodine receptor mRNAs were correlated positively with left ventricular fractional shortening (r=0.73, P<0.0001 and r=0.61, P<0.01 respectively). Attenuation of the decrease in left ventricular fractional shortening occurred on treatment with TCV-116. After the treatment with TCV-116, the levels of SERCA and phospholamban mRNAs were restored to the respective values in sham-operated rats. Ryanodine receptor mRNA levels remained unchanged after treatment with TCV-116. These results indicate that the down-regulation of SERCA and ryanodine receptor mRNA levels may be related to cardiac dysfunction in the volume-overloaded heart. In addition, treatment with an angiotensin II receptor antagonist may restore the altered sarcoplasmic reticulum mRNA levels to control levels, and this may result in attenuation of the functional impairment in the volume-overloaded heart.  (+info)

Effects of angiotensin II receptor blockade on proximal fluid uptake in the rat kidney. (8/2330)

Angiotensin II has a well described dose-dependent biphasic action on proximal tubule fluid uptake, although the concentration and effect of endogenous luminal angiotensin II remain controversial. Shrinking split-droplet micropuncture was used to examine the fluid uptake in response to the luminal application of three AT1 antagonists (losartan, EXP3174, candesartan). Addition of losartan at 10(-8) M decreased fluid uptake rate (Jva) by 17.5+/-2.2% (P<0.05). Luminal addition of EXP3174 at concentrations between 10(-9)-10(-5) M caused a dose-dependent decrease in fluid uptake, with a maximum decrease of 41.0+/-9.5% (P<0.01) at 10(-6) M. Candesartan also decreased fluid uptake, by 21.9+/-4.9% (P<0.05) at 10(-8) M and 23.6+/-5.5% (P<0.05) at 10(-5) M. All three antagonists at a low concentration (10(-8) M) decreased fluid uptake. EXP3174 and candesartan at a higher concentration (10(-5) M) also decreased fluid uptake in contrast to the previously reported effect of losartan. We conclude that the endogenous concentration of antiotensin II in the proximal luminal fluid is low and exerts a stimulatory effect on fluid absorption. Losartan at concentrations greater than 10(-6) M may have a non-selective action on fluid uptake.  (+info)

Tetrazoles are a class of heterocyclic aromatic organic compounds that contain a five-membered ring with four nitrogen atoms and one carbon atom. They have the chemical formula of C2H2N4. Tetrazoles are stable under normal conditions, but can decompose explosively when heated or subjected to strong shock.

In the context of medicinal chemistry, tetrazoles are sometimes used as bioisosteres for carboxylic acids, as they can mimic some of their chemical and biological properties. This has led to the development of several drugs that contain tetrazole rings, such as the antiviral drug tenofovir and the anti-inflammatory drug celecoxib.

However, it's important to note that 'tetrazoles' is not a medical term per se, but rather a chemical term that can be used in the context of medicinal chemistry or pharmacology.

Hydrogels are defined in the medical and biomedical fields as cross-linked, hydrophilic polymer networks that have the ability to swell and retain a significant amount of water or biological fluids while maintaining their structure. They can be synthesized from natural, synthetic, or hybrid polymers.

Hydrogels are known for their biocompatibility, high water content, and soft consistency, which resemble natural tissues, making them suitable for various medical applications such as contact lenses, drug delivery systems, tissue engineering, wound dressing, and biosensors. The physical and chemical properties of hydrogels can be tailored to specific uses by adjusting the polymer composition, cross-linking density, and network structure.

Click chemistry is a term used to describe a group of chemical reactions that are fast, high-yielding, and highly selective. These reactions typically involve the formation of covalent bonds between two molecules in a simple and efficient manner, often through the use of a catalyst. The concept of click chemistry was first introduced by K. B. Sharpless, who won the Nobel Prize in Chemistry in 2001 for his work on chiral catalysis.

In the context of medical research and drug development, click chemistry has emerged as a valuable tool for rapidly synthesizing and optimizing small molecule compounds with therapeutic potential. By using click chemistry reactions to quickly and efficiently link different chemical building blocks together, researchers can rapidly generate large libraries of potential drug candidates and then screen them for biological activity. This approach has been used to discover new drugs for a variety of diseases, including cancer, infectious diseases, and neurological disorders.

One common type of click chemistry reaction is the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, which involves the reaction between an azide and an alkyne to form a triazole ring. This reaction is highly selective and can be carried out under mild conditions, making it a popular choice for chemical synthesis in the life sciences. Other types of click chemistry reactions include the Diels-Alder cycloaddition, the thiol-ene reaction, and the Staudinger ligation.

Overall, click chemistry has had a significant impact on medical research and drug development by enabling the rapid and efficient synthesis of complex small molecule compounds with therapeutic potential. Its versatility and selectivity make it a powerful tool for researchers seeking to discover new drugs and better understand the molecular mechanisms underlying human disease.

Alkenes are unsaturated hydrocarbons that contain at least one carbon-carbon double bond in their molecular structure. The general chemical formula for alkenes is CnH2n, where n represents the number of carbon atoms in the molecule.

The double bond in alkenes can undergo various reactions, such as addition reactions, where different types of molecules can add across the double bond to form new compounds. The relative position of the double bond in the carbon chain and the presence of substituents on the carbon atoms can affect the physical and chemical properties of alkenes.

Alkenes are important industrial chemicals and are used as starting materials for the synthesis of a wide range of products, including plastics, resins, fibers, and other chemicals. They are also found in nature, occurring in some plants and animals, and can be produced by certain types of bacteria through fermentation processes.

Polyethylene glycols (PEGs) are a family of synthetic, water-soluble polymers with a wide range of molecular weights. They are commonly used in the medical field as excipients in pharmaceutical formulations due to their ability to improve drug solubility, stability, and bioavailability. PEGs can also be used as laxatives to treat constipation or as bowel cleansing agents prior to colonoscopy examinations. Additionally, some PEG-conjugated drugs have been developed for use in targeted cancer therapies.

In a medical context, PEGs are often referred to by their average molecular weight, such as PEG 300, PEG 400, PEG 1500, and so on. Higher molecular weight PEGs tend to be more viscous and have longer-lasting effects in the body.

It's worth noting that while PEGs are generally considered safe for use in medical applications, some people may experience allergic reactions or hypersensitivity to these compounds. Prolonged exposure to high molecular weight PEGs has also been linked to potential adverse effects, such as decreased fertility and developmental toxicity in animal studies. However, more research is needed to fully understand the long-term safety of PEGs in humans.

According to the medical definition, ultraviolet (UV) rays are invisible radiations that fall in the range of the electromagnetic spectrum between 100-400 nanometers. UV rays are further divided into three categories: UVA (320-400 nm), UVB (280-320 nm), and UVC (100-280 nm).

UV rays have various sources, including the sun and artificial sources like tanning beds. Prolonged exposure to UV rays can cause damage to the skin, leading to premature aging, eye damage, and an increased risk of skin cancer. UVA rays penetrate deeper into the skin and are associated with skin aging, while UVB rays primarily affect the outer layer of the skin and are linked to sunburns and skin cancer. UVC rays are the most harmful but fortunately, they are absorbed by the Earth's atmosphere and do not reach the surface.

Healthcare professionals recommend limiting exposure to UV rays, wearing protective clothing, using broad-spectrum sunscreen with an SPF of at least 30, and avoiding tanning beds to reduce the risk of UV-related health problems.

Alkynes are a type of hydrocarbons that contain at least one carbon-carbon triple bond in their molecular structure. The general chemical formula for alkynes is CnH2n-2, where n represents the number of carbon atoms in the molecule.

The simplest and shortest alkyne is ethyne, also known as acetylene, which has two carbon atoms and four hydrogen atoms (C2H2). Ethyne is a gas at room temperature and pressure, and it is commonly used as a fuel in welding torches.

Alkynes are unsaturated hydrocarbons, meaning that they have the potential to undergo chemical reactions that add atoms or groups of atoms to the molecule. In particular, alkynes can be converted into alkenes (hydrocarbons with a carbon-carbon double bond) through a process called partial reduction, or they can be fully reduced to alkanes (hydrocarbons with only single bonds between carbon atoms) through a process called complete reduction.

Alkynes are important intermediates in the chemical industry and are used to produce a wide range of products, including plastics, resins, fibers, and pharmaceuticals. They can be synthesized from other hydrocarbons through various chemical reactions, such as dehydrogenation, oxidative coupling, or metathesis.

Methacrylates are a group of chemical compounds that contain the methacrylate functional group, which is a vinyl group (CH2=CH-) with a carbonyl group (C=O) at the β-position. This structure gives them unique chemical and physical properties, such as low viscosity, high reactivity, and resistance to heat and chemicals.

In medical terms, methacrylates are used in various biomedical applications, such as dental restorative materials, bone cements, and drug delivery systems. For example, methacrylate-based resins are commonly used in dentistry for fillings, crowns, and bridges due to their excellent mechanical properties and adhesion to tooth structures.

However, there have been concerns about the potential toxicity of methacrylates, particularly their ability to release monomers that can cause allergic reactions, irritation, or even mutagenic effects in some individuals. Therefore, it is essential to use these materials with caution and follow proper handling and safety protocols.

The delocalization energy in tetrazole is 209 kJ/mol. 1H-Tetrazole and 5-(benzylthio)-1H-tetrazole (BTT) are widely used as ... A well-known tetrazole is dimethyl thiazolyl diphenyl tetrazolium bromide (MTT). This tetrazole is used in the MTT assay to ... Other tetrazoles are used for their explosive or combustive properties, such as tetrazole itself and 5-aminotetrazole, which ... Three isomers of the parent tetrazole exist, differing in the position of the double bonds: 1H-, 2H-, and 5H-tetrazole. The 1H ...
The base acids, 5-azido-1H-tetrazole and 5-azido-2H-tetrazole both can exist. The 1H version has a hydrogen atom bonded to a ... The ion is made by removing a proton from 5-azido-1H-tetrazole. The molecular structure contains a five-membered ring with four ... Zhaoxu, Chen; Jianfen, Fan; Heming, Xiao (January 1999). "Theoretical study on tetrazole and its derivatives. Part 7: ab initio ... "5-Azido-1H-tetrazole - Improved Synthesis, Crystal Structure and Sensitivity Data". Zeitschrift für anorganische und allgemeine ...
In addition, the binding to the target enzyme is pH-sensitive, and the negatively-charged tetrazole ring, which is similar in ... Noda K, Saad Y, Kinoshita A, Boyle TP, Graham RM, Husain A, Karnik SS (February 1995). "Tetrazole and carboxylate groups of ... "see negatively charged tetrazole structure". Archived from the original on 22 January 2021. Retrieved 21 October 2017. " ... Losartan is generally marketed as the (basic) potassium salt of the aromatized negatively charged tetrazole, called "losartan ...
One pathway is from oxidation of tetrazoles in the presence of aldehydes. Similarly, the reaction of tetrazoles with acyl ... 4-Oxadiazoles via Di-tert-butyl Peroxide Promoted Acylation of Aryl Tetrazoles with Aldehydes". The Journal of Organic ...
Tetrazoles from Nitriles in Water †". The Journal of Organic Chemistry. 66 (24): 7945-7950. doi:10.1021/jo010635w. ISSN 0022- ...
Tetrazoles: Building Blocks for Peptide Surrogates". J. Org. Chem. 77 (2): 1174-1180. doi:10.1021/jo2022235. PMID 22171684. "A ...
Synthesis of Monosubstituted Tetrazoles". The Journal of Organic Chemistry. 15 (5): 1082-1092. doi:10.1021/jo01151a027. ISSN ...
The tetrazole represents a non-classical bio-isostere. The carboxylate seen in the molecule is the active moiety after the ... An interesting aspect of the molecule is that unlike other ARBs which have a tetrazole attached to the molecule, Azilsartan has ...
Design, Synthesis, and Functional Evaluation of 1, 5-Disubstituted Tetrazoles as Monoamine Neurotransmitter Reuptake Inhibitors ... Tetrazoles (ROK): 10dl (CID:118713802) (S/N/D 7.6/45.2/330nM): 2at (CID:118706539): THIQ Derivatives: AN12 (CID:10380161): ... synthesis and structure-activity relationship of benzylpiperidine-tetrazoles". Bioorganic & Medicinal Chemistry. 25 (20): 5278- ...
These sartan medicines have a specific ring structure (tetrazole) whose synthesis could potentially lead to the formation of ... "Risk of presence of mutagenic azido impurities in sartan active substances with a tetrazole ring" (Press release). European ... "Angiotensin-II-receptor antagonists (sartans) containing a tetrazole group". European Medicines Agency (EMA). 17 September 2018 ... in tetrazole-containing sartans. In September 2021, the EDQM announced that investigations had revealed a novel azido ...
The azide is in equilibrium with the tetrazole 3. Lahti, Paul M.; Esat, Burak; Liao, Yi; Serwinski, Paul; Lan, Jiang; Walton, ...
This set contains pyrrole, imidazole, pyrazole, triazoles, tetrazole, and pentazole. Substituted analogs of pentazole are ... Tetrazole, and Pentazole Rings: Release of Parent Azoles. Generation of Unstable Pentazole, HN5/N5-, in Solution" (PDF). The ... tetrazole and application of the methodology to 1-(p-methoxyphenyl) pentazole". Chemical Communications (8): 1016-1017. doi: ...
Tetrazoles and tetrazolidines are pivotal parts of the "sartan" class of hypertensives, e.g. Candesartan cilexetil (candesartan ...
This tetrazole explosive has a decomposition temperature of 124 °C. It is very sensitive, with impact sensitivity lower than ... The C2N14 molecule is a monocyclic tetrazole with three azide groups. This ring form is in equilibrium with isocyanogen ... which at room temperature quickly undergoes an irreversible cyclization reaction to form a tetrazole ring. ... tetraazide, an isomeric acyclic structure that has long been known to cyclize quickly to the tetrazole. It is one of a family ...
... antimicrobial activity and anti-biofilm activity of novel tetrazole derivatives". Heterocyclic Communications. 23 (4): 325-330 ...
... s were first observed in the thermal decomposition of 2-tetrazoles releasing nitrogen: Nitrilimines are linear 1,3- ... 5-Disubstituted Tetrazoles". The Journal of Organic Chemistry. 24 (6): 892-893. doi:10.1021/jo01088a034. (Functional groups). ...
MTT, a yellow tetrazole, is reduced to purple formazan in living cells. A solubilization solution (usually either dimethyl ...
In the Julia-Kocienski olefination[16] the alkylating agent is a tetrazole. It proceeds with the same mechanism as the ...
Nitro blue tetrazolium is a chemical compound composed of two tetrazole moieties. It is used in immunology for sensitive ...
Tetrazoles contain a pair of double-bonded nitrogen atoms with oxidation state 0 in the ring. A Synthesis of the parent 1H- ... tetrazole, CH2N4 (two atoms N(0)) is given in Henry, Ronald A.; Finnegan, William G. (1954). "An Improved Procedure for the ...
Tetrazoles contain a pair of double-bonded nitrogen atoms with oxidation state 0 in the ring. A Synthesis of the parent 1H- ... tetrazole, CH2N4 (two atoms N(0)) is given in Ronald A. Henry and William G. Finnegan, "An Improved Procedure for the ...
N.B There are some alternative ways of making the tetrazole ring however; C.f. the sartan drugs synthesis schemes. Bu3SnN3 is a ...
Examples of tetrazol-5-ylidenes based on tetrazole have been prepared by Araki. The N1 and N3 positions are substituted with ...
Squires RF, Saederup E, Crawley JN, Skolnick P, Paul SM (1984). "Convulsant potencies of tetrazoles are highly correlated with ...
Lakshman Mahesh K., Singh Manish K., Parrish Damon, Balachandran Raghavan, Day Billy W. (2010). "Azide−Tetrazole Equilibrium of ... such as organic azides and tetrazoles, or mesoionic münchnone and acylamino ketene. Valence tautomerism requires a change in ...
In 2011, azobis(tetrazole) was prepared by Klapötke and Piercey which has a ten-nitrogen chain. The record was later taken by a ... Klapötke, Thomas M.; Piercey, Davin G. (2011). "1,1′-Azobis(tetrazole): A Highly Energetic Nitrogen-Rich Compound with a N10 ...
It is a reagent used in the synthesis of tetrazoles, which in turn are used to generate angiotensin II receptor antagonists. In ... Click Chemistry for the Synthesis of 5-Substituted Tetrazoles from Organoaluminum Azides and Nitriles". Angewandte Chemie. 119 ...
The medicine has an extended diphenyl group with a tetrazole at the 2-prime position. At the 4'prime position, the molecule has ... Tetrazoles, Biphenyls, Lactams, Spiro compounds, Nitrogen heterocycles, Wikipedia medicine articles ready to translate). ...
Klapötke, Thomas M.; Piercey, Davin G. (2011-04-04). "1,1′-Azobis(tetrazole): A Highly Energetic Nitrogen-Rich Compound with a ...
"Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor- ...
The delocalization energy in tetrazole is 209 kJ/mol. 1H-Tetrazole and 5-(benzylthio)-1H-tetrazole (BTT) are widely used as ... A well-known tetrazole is dimethyl thiazolyl diphenyl tetrazolium bromide (MTT). This tetrazole is used in the MTT assay to ... Other tetrazoles are used for their explosive or combustive properties, such as tetrazole itself and 5-aminotetrazole, which ... Three isomers of the parent tetrazole exist, differing in the position of the double bonds: 1H-, 2H-, and 5H-tetrazole. The 1H ...
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STUDIES WITH TETRAZOLE DERIVATIVES. IV. Some Pharmacologic Properties Of Aminomethyl Tetrazoles. E. G. GROSS and R. M. ... STUDIES WITH TETRAZOLE DERIVATIVES Message Subject (Your Name) has forwarded a page to you from Journal of Pharmacology and ... The effect on the central nervous system of 38 derivatives of aminomethyl tetrazole has been studied. This group of compounds ... Some Pharmacologic Properties Of Aminomethyl Tetrazoles. Abstract. ...
Synthesis and characterization of new 1N and 2N-substituted tetrazoles applicable for Energetic Coordination Compounds and ... Synthesis and characterization of new 1N and 2N-substituted tetrazoles applicable for Energetic Coordination Compounds and ... Kofen, Moritz (2022): Synthesis and characterization of new 1N and 2N-substituted tetrazoles applicable for Energetic ...
In situ forming hydrogels were developed from 4-arm poly(ethylene glycol)?methacrylate (PEG-4-MA) and ?tetrazole (PEG-4-Tet) ... The cell experiments via an indirect contact assay demonstrated that these "tetrazole?alkene" photo-click PEG hydrogels were ... These results confirm that "tetrazole?alkene" photo-click reaction is. highly compatible with these loaded proteins. This photo ... In Situ Forming Hydrogels via Catalyst-Free and Bioorthogonal "Tetrazole-Alkene" Photo-Click Chemistry ...
... showing that the tetrazole could initiate assembly of the TIR1 auxin co-receptor complex. We then tested the tetrazoles ... The tetrazole analogue of the auxin indole-3-acetic acid binds preferentially to TIR1 and not AFB5 ... 9 more authors) (2018) The tetrazole analogue of the auxin indole-3-acetic acid binds preferentially to TIR1 and not AFB5. ACS ... The basis of the preference of indole-3-tetrazole for TIR1 was revealed to be a single residue substitution using molecular ...
Practical synthesis of (S)-pyrrolidin-2-yl-1H-tetrazole, incorporating efficient protecting group removal by flow-reactor ... Practical synthesis of (S)-pyrrolidin-2-yl-1H-tetrazole, incorporating efficient protecting group removal by flow-reactor ...
Suppliers of Tetrazoles in India, we use latest technology to produce high quality Tetrazoles. We are a manufacturer.... ... Tetrazoles Manufacturers In India , Tetrazolessuppliers In India - Corvine Chemicals. October 1, 2021 ⚊ 1 Min read ⚊ Views 167 ... Corvine Chemicals is the largest manufacturer & Suppliers of Tetrazoles in India, we use latest technology to produce high ... quality Tetrazoles. We are a manufacturer since 1988 that offers custom manufacturing services for specialty chemicals with ISO ...
Synthesis of fused tetrazole derivatives via a tandem cycloaddition and N-allylation reaction and parallel synthesis of fused ... Synthesis of fused tetrazole derivatives via a tandem cycloaddition and N-allylation reaction and parallel synthesis of fused ... A method for the synthesis of novel fused tricyclic tetrazoles from allylic bromides generated by the recently discovered ...
5-(4-bromophenyl)-1-(tetrahydro-2H-pyran-2-yl)tetrazole. Product Code: BM678 ...
For more information such as price, delivery, product specification and MSDS please contact us ...
Corvine chemicals is the Leading Manufacturers and suppliers of Tetrazole in India. Widest Range of Tetrazolesare availlable & ... Tags: sodium azide manufacturers in india, tetrazoles manufacturers in india Best Dofollow Social Bookmarking Websites List ... Tetrazoles Manufacturers In India , Sodium Azide Manufacturers - Corvine Chemicals. Submitted by creative junior , October 6, ... Corvine chemicals is the Leading Manufacturers and suppliers of Tetrazole in India. Widest Range of Tetrazolesare availlable & ...
2H-Tetrazole-5-acetic acid, hydrazide. CAS Number: 1002104-07-5. Catalog Number: 1P0001Q0. MDL Number: MFCD18071020. Molecular ... Synonyms: Tetrazole-5-acetohydrazide; 1002104-07-5; 2H-Tetrazole-5-acetic acid, hydrazide; MCULE-5629806431; TRA0008334; AS- ... Keywords: 1002104-07-5,MFCD18071020,1P0001Q0,2H-Tetrazole-5-acetic acid, hydrazide,C3H6N6O ... 31945; SY011683; (1H-Tetrazole-5-yl)acetic acid hydrazide; 2-(1h-tetrazol-5-yl)acetic acid hydrazide; DB-058328; TC-308784; FT- ...
Tetrazoles / pharmacology * Tetrazoles / therapeutic use* * Ticlopidine / analogs & derivatives * Ticlopidine / therapeutic use ...
tetrazole group Archives - European Industrial Pharmacists Group (EIPG). Home / Revision of the CDMhs Q&As document on ... Four different conditions (A-D) are set for the marketing authorisation (MA) of tetrazole sartans, with specific dates to be ... 31 referral on angiotensin-II-receptor antagonists (sartans) containing a tetrazole group. According to the indications ... tetrazole group, type IA C.I.11.a variation, type IB C.I.11.z variation ...
Best Quality,Quick Response,Lower Price. Serving cas 14677-11-3, Formula C9H6 N4,triazole-carbonitrile.
Organotin-functionalised poly(tetrazoles), including the supramolecular structure of 1,6-(2-Bu 3 SnN 4 C) 2 (CH 2 ) 6. Journal ... Organotin-functionalised poly(tetrazoles), including the supramolecular structure of 1,6-(2-Bu 3 SnN 4 C) 2 (CH 2 ) 6. In: ... Organotin-functionalised poly(tetrazoles), including the supramolecular structure of 1,6-(2-Bu 3 SnN 4 C) 2 (CH 2 ) 6. / ... Organotin-functionalised poly(tetrazoles), including the supramolecular structure of 1,6-(2-Bu 3 SnN 4 C) 2 (CH 2 ) 6. ...
van Hoek, A. Synthesis of an arginase inhibitor using the Ugi-tetrazole reaction. Bachelors Project, Pharmacy. ...
Dive into the research topics of Highly asymmetric coordination of trimethylsilyl groups to tetrazole and triazole rings: an ... 1-Trimethylsilyltetrazole, 1, has been synthesised from chlorotrimethylsilane and tetrazole in the presence of triethylamine as ... T1 - Highly asymmetric coordination of trimethylsilyl groups to tetrazole and triazole rings: an experimental and computational ... Highly asymmetric coordination of trimethylsilyl groups to tetrazole and triazole rings: an experimental and computational ...
... Optimization and SAR research at the benzoxazole and tetrazole rings of JNJ4796 as new ant ... we described the structure-activity relationship of the benzoxazole and tetrazole rings of JNJ4796. Many derivatives ...
Keywords: Quinoline, benzimidazole, benzoxazole, benzothiazole, azetidin-2one, thiazolidin-4-one, tetrazole. PDF Version ... tetrazole nuclei. The newly synthesized compounds were characterized by elemental analysis and IR, 1H-NMR, 13C NMR and mass ...
Categories: Tetrazoles Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, CopyrightRestricted 1 images ...
Of the three, only the tetrazoles show promise as useful monomers. A series of polymers which possessed moderate viscosities, ... Three 1,3-dipole presursors, the sydnone, the hydrazide chloride, and the tetrazole systems were studied in terms of their ... Three 1,3-dipole presursors, the sydnone, the hydrazide chloride, and the tetrazole systems were studied in terms of their ... Of the three, only the tetrazoles show promise as useful monomers. A series of polymers which possessed moderate viscosities, ...
Hi Tetrazole,. The Viceroy and Monarch comparison is a much welcomed addition to our site as is the image of the mating Cabbage ...
2H-tetrazole 3H-diazirine 4-iminobutane-1,2,3-triol 5H-tetrazole ...
... a tetrazole-based lanosterol 14α-demethylase inhibitor; APX001, which interrupts glycosylphosphatidylinositol biosynthesis by ...
Tetrazole. *Carboxylic acid derivative. *Carboxylic acid. *Monocarboxylic acid or derivatives. *Azacycle. *Organoheterocyclic ...
by Tetrazole Fri Aug 26, 2022 11:09 pm. * Best looking cactus variety for a medusa head planter? Last post by cactiguy2022 « ...
J02AC Triazole and tetrazole derivatives. All oral and parenteral formulations of fluconazole are classified here. ...
All CEP dossiers for sartans containing a tetrazole ring have been updated to address the potential presence of nitrosamines in ... September 2018: Investigation extended to sartans with a tetrazole ring. February 2019: CHMP Article 31 referral report ... Eur.) Commission published five revised monographs on sartans containing a tetrazole ring (Valsartan, Losartan potassium, ... published: companies to review manufacturing processes to avoid presence of nitrosamine impurities in sartans with a tetrazole ...
  • Some tetrazole derivatives with high energy have been investigated as high performance explosives as a replacement for TNT and also for use in high performance solid rocket propellant formulations. (wikipedia.org)
  • The effect on the central nervous system of 38 derivatives of aminomethyl tetrazole has been studied. (aspetjournals.org)
  • In situ forming hydrogels were developed from 4-arm poly(ethylene glycol)?methacrylate (PEG-4-MA) and ?tetrazole (PEG-4-Tet) derivatives through catalyst-free and bioorthogonal "tetrazole?alkene" photo-click chemistry. (polymer.cn)
  • Variety of tetrazole derivatives, including antihypertensive pharmaceutical agent Irbesartan, are produced using alkali metal azides (MeN 3 ). (news-medical.net)
  • Djandjighian, L Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers. (bindingdb.org)
  • Treatment of organic nitriles with sodium azide in the presence of iodine or silica-supported sodium bisulfate as a heterogeneous catalyst enables an advantageous synthesis of 5-substituted 1H-tetrazoles. (wikipedia.org)
  • 1H-Tetrazole and 5-(benzylthio)-1H-tetrazole (BTT) are widely used as acidic activators of the coupling reaction in oligonucleotide synthesis. (wikipedia.org)
  • A method for the synthesis of novel fused tricyclic tetrazoles from allylic bromides generated by the recently discovered DiazAll reaction has been developed. (lu.se)
  • Design and Synthesis of High-Performance Planar Explosives and Solid Propellants with Tetrazole Moieties S. Lal, R.J. Staples, J.M. Shreeve Org. (msu.edu)
  • 1H-Tetrazole was first prepared by the reaction of anhydrous hydrazoic acid and hydrogen cyanide under pressure. (wikipedia.org)
  • 2-Aryl-2H-tetrazoles are synthesized by a [3+2] cycloaddition reaction between an aryl diazonium and trimethylsilyldiazomethane. (wikipedia.org)
  • Tetrazole based energetic materials produce high-temperature, non-toxic reaction products such as water and nitrogen gas, and have a high burn rate and relative stability, all of which are desirable properties. (wikipedia.org)
  • These results confirm that "tetrazole?alkene" photo-click reaction is highly compatible with these loaded proteins. (polymer.cn)
  • This tetrazole compound was used to develop a selective screen by exposing E. coli hosts to the compound and exposing the cells to UV light to induce the photoclick reaction of the tetrazole compound binding to the terminal alkene on botryococcene. (plu.edu)
  • The cell experiments via an indirect contact assay demonstrated that these "tetrazole?alkene" photo-click PEG hydrogels were noncytotoxic. (polymer.cn)
  • Three 1,3-dipole presursors, the sydnone, the hydrazide chloride, and the tetrazole systems were studied in terms of their usefulness as monomers for 1,3- dipolar addition reactions. (dtic.mil)
  • Optimization and SAR research at the benzoxazole and tetrazole rings of JNJ4796 as new anti-influenza A virus agents, part 2. (bvsalud.org)
  • In this study, we described the structure-activity relationship of the benzoxazole and tetrazole rings of JNJ4796. (bvsalud.org)
  • Corvine Chemicals is the largest manufacturer & Suppliers of Tetrazoles in India, we use latest technology to produce high quality Tetrazoles. (kaancy.com)
  • Corvine chemicals is the Leading Manufacturers and suppliers of Tetrazole in India. (segut.com)
  • The name tetrazole also refers to the parent compound with formula CH2N4, of which three isomers can be formulated. (wikipedia.org)
  • This tetrazole is used in the MTT assay to quantify the respiratory activity of live cells culture, although it generally kills the cells in the process. (wikipedia.org)
  • The basis of the preference of indole-3-tetrazole for TIR1 was revealed to be a single residue substitution using molecular docking, and assays using tir1 and afb5 mutant lines confirmed selectivity in vivo. (whiterose.ac.uk)
  • Improved affinity for TIR1 and the preference for binding to TIR1 was maintained for 4- and 6-chloroindole-3-tetrazoles, coupled with improved efficacy in vivo. (whiterose.ac.uk)
  • Tetrazoles are a class of synthetic organic heterocyclic compound, consisting of a 5-member ring of four nitrogen atoms and one carbon atom. (wikipedia.org)
  • Angiotensin II receptor blockers - such as losartan and candesartan, often are tetrazoles. (wikipedia.org)
  • There are several pharmaceutical agents which are tetrazoles, including several cephalosporin-class antibiotics. (wikipedia.org)
  • sartans) containing a tetrazole group . (eipg.eu)
  • A previously developed tetrazole compound is able to photoclick onto terminal alkenes and produce a fluorescent adduct. (plu.edu)
  • 2-Tetrazoles can undergo controlled thermal decomposition to form highly reactive nitrilimines. (wikipedia.org)
  • R.sub.1 is --CH.sub.2 COOH or methyl tetrazole, and X.sub.1 and X.sub.2 are each a halogen or loweralkyl, or when taken together form with the two attached carbons a phenyl ring.These compounds are useful as antihypertensive agents, diuretics and uricosuric agents. (justia.com)
  • Tetrazoles can act as bioisosteres for carboxylate groups because they have similar pKa and are deprotonated at physiological pH. (wikipedia.org)
  • Four different conditions (A-D) are set for the marketing authorisation (MA) of tetrazole sartans, with specific dates to be met for their fulfilment by marketing authorisation holders (MAHs). (eipg.eu)
  • Substituted heteroaryl aldehyde ( 3a , b ) was synthesized from 5-chloro-3-methyl-1-phenyl-1 H -pyrazole-4-methyl-carbaldehyde on protection with ethylene glycol followed by treatment with 4-amino triazole/5-amino tetrazole and then deprotection using acid. (nih.gov)
  • Combination of Energetic Tetrazole and Triazole: Promising Materials with Exceptional Stability and Low Mechanical Sensitivity as Propellants and Gas Generators. (nih.gov)
  • Angiotensin II receptor blockers - such as losartan and candesartan, often are tetrazoles. (wikipedia.org)
  • The 1 H -tetrazole function is a key structural component of cardiovascular drugs such as sartans (losartan, valsartan, etc). (thieme.de)
  • Inquire Ethyl Tetrazole-5-carboxylate (cas: 55408-10-1 ) online by filling out the inquiry form, we will get back to you within 24 hours! (musechem.com)
  • 1. Enzymatic hydrolysis of esters containing a tetrazole ring. (nih.gov)
  • Selective cleavage of substituted N -trityl-protected tetrazoles is easily performed with indium metal and methanol under Reflux" explained Professor Yus. (thieme.de)
  • 1 H -Tetrazoles are privileged structures in medicinal chemistry and drug discovery: they can be found in a number of bioactive compounds and drugs, and this moiety can also be used as a carboxylic group bioisosteric replacement. (thieme.de)
  • The formulation aims to result in higher yields and lower overall operational costs compared to traditional Tetrazole activator solutions. (outsourcing-pharma.com)
  • This tetrazole is used in the MTT assay to quantify the respiratory activity of live cells culture, although it generally kills the cells in the process. (wikipedia.org)
  • 2. Tetrazole activity against Candida albicans. (nih.gov)
  • 16. New 1,5 and 2,5-disubstituted tetrazoles-dependent activity towards surface barrier of Candida albicans. (nih.gov)
  • The groups of Professors Miguel Yus and Cherif Behloul have recently reported a new efficient method for cleaving the trityl group from 1 H -tetrazoles, which showed excellent selectivity and orthogonality. (thieme.de)
  • The 1H- and 2H- isomers are tautomers, with the equilibrium lying on the side of 1H-tetrazole in the solid phase. (wikipedia.org)
  • Crystal structure determination at 2.3 A of recombinant human dihydrofolate reductase ternary complex with NADPH and methotrexate-gamma-tetrazole. (rcsb.org)
  • The tetrazole-functionalised calixdiquinone 5,17-di-tert-butyl-26,28-bis-(1H-tetrazole-5-ylmethoxy)-calix[4]-25,27-diquinone Q was synthesised by chemical oxidation of the bis-tetrazole calix[4]arene precursor using PbO2/HClO4. (edu.au)