Molecules synthesis piperazines. Medical search. Frequent questions

The present review focuses on the synthesis and application of different piperazine derivatives and their metal complexes having diverse applications. (rsc.org)
The Tungsten-Promoted Synthesis of Piperidyl-Modified erythro-Methylphenidate Derivatives. (acs.org)
Design, synthesis, biological evaluation, and molecular modeling of coumarin-piperazine derivatives as acetylcholinesterase inhibitors. (journals.cz)
Regioselective Synthesis of Mono- and Dispiropyrazoline Derivatives via 1,3-dipolar Cycloaddition with Nitrilimines. (icmub.com)
Akin, Synthesis of 1, 2, 4-triazole-5-on derivatives and determination of carbonic anhydrase II isoenzyme inhibition effects, Bioorg. (dntb.gov.ua)
Sağlık, Synthesis, molecular docking analysis and carbonic anhydrase I-II inhibitory evaluation of new sulfonamide derivatives, Bioorg. (dntb.gov.ua)

The piperazine scaffold is a privileged structure frequently found in biologically active compounds. (rsc.org)
This is one of the reasons why piperazine based compounds are gaining prominence in today's research. (rsc.org)
Piperazine ring-based compounds find their application in biological systems with antihistamine, anticancer, antimicrobial and antioxidant properties. (rsc.org)
Herein, to achieve efficient delivery of negatively charged siRNA duplexes, the internal cavity of "humanized"chimeric Archaeal ferritin (HumAfFt) was specifically decorated with novel cationic piperazine-based compounds (PAs). (unicatt.it)
High potency was predominantly achieved by piperidine and piperazine substitutions, whereupon three compounds were identified as promising candidates, showing preferable metabolic stability. (ilrs.de)
Based on PASS predictions for ~250000 molecules from the Open NCI database, we selected compounds with potential anti-angiogenesis action. (way2drug.com)
The tri-component synthesis of novel chiral benzimidazole Mannich bases, by reaction between benzimidazole, aqueous 30% formaldehyde and an amine, the biological evaluation and DFT studies of the new compounds are reported here. (biomedcentral.com)
The planarity of the molecules, specific bond lengths and localization of HOMO-LUMO orbitals is responsible for the best biological activities of the compounds. (biomedcentral.com)

The finding of heterocyclic alkanes with destructive quantum interference charts a pathway for chemical design of short molecular insulators using organic molecules. (rsc.org)
In this article, we examine the single-molecule junction properties of saturated heterocyclic cyclohexane derivates, 1,4- dithiane , 1,4- piperazine and 1,4-diazabicyclo[2.2.2]octane, C222-diaza , also known as DABCO, shown in Scheme 1 . (rsc.org)
1-(Methyl-D3)piperazine 2HCl, a remarkable chemical compound, is characterized by its deuterium-labeled methyl group and its association with piperazine, a bicyclic heterocyclic amine. (clearsynth.com)
In addition to offering an attractive collection of heterocyclic building blocks and fragments, Avistron also offers bespoke services in the areas of intermediate and library compound synthesis. (avistronchemistry.com)
Pyridine and piperidine are the most frequently occurring heterocyclic building blocks in drug molecules. (chemenu.com)

Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4′-halophenyl)nortropanes: Candidate Radioligands for In Vivo Imaging of the Brain Dopamine Transporter with Positron Emission Tomography. (acs.org)
Synthesis and Biological Evaluation of Bupropion Analogues as Potential Pharmacotherapies for Cocaine Addiction. (acs.org)
Reddy, Synthesis and biological evaluation of pyrazolo-triazole hybrids as cytotoxic and apoptosis inducing agents, Org. (dntb.gov.ua)

Synthesis of novel 5-HT1A arylpiperazine ligands: Binding data and computer-aided analysis of pharmacological potency. (ac.rs)
A series of multi-target-directed ligands (MTDLs), obtained by attachment of a hydroxyphenylbenzimidazole (BIM) unit to donepezil (DNP) active mimetic moiety (benzyl-piperidine/-piperazine) was designed, synthesized, and evaluated as potential anti-Alzheimer's disease (AD) drugs in terms of biological activity (inhibition of acetylcholinesterase (AChE) and β-amyloid (Aβ) aggregation), metal chelation, and neuroprotection capacity. (uc.pt)
In the broadest sense, Peptidomimetics are organic molecules which mimic some properties of natural peptide ligands. (ijpsr.com)

Piperazine-derived small molecules as potential Flaviviridae NS3 protease inhibitors. (us.es)

Designing highly insulating sub-nanometer molecules is difficult because tunneling conductance increases exponentially with decreasing molecular length. (rsc.org)
13-17 This opens a potential avenue for using molecules with destructive σ-interference as molecular insulators. (rsc.org)
These molecules all have molecular length below 5 Å, and thus constitute some of the shortest that can be measured in Au-molecule-Au junctions. (rsc.org)
Molecular imprinting is a process in which functional and crosslinking monomers are co-polymerized in the presence of the target analyte, the imprint molecule. (intechopen.com)
Synthesis, spectroscopic, cyclic voltammetry properties and molecular structure of the thiocyanato-N meso-tetratolylporphyrinato zinc(II) ion complex. (icmub.com)

In most antidepressants, a piperazine-based structural motif can be identified as a common moiety. (ac.rs)
The docking pose of the studied LA1 molecule depends of the protonated state of the nitrogen atom of the piperazine moiety where in the best scored poses, the xanthine moiety of LA1 is bound into the catalytic active site (CAS) of AChE, while the arylpiperazine fragment is placed into the peripheral binding site (PAS). (journals.cz)

Variants of the azlactone synthesis in which analogues of azlactones are used are sometimes advantageous. (wikipedia.org)
Synthesis of analogues showing activity in in vitro assay on Kv1.5 potassium ion channel was described in the literature, which is validated biological target in the treatment of arrhythmia. (unizg.hr)

They are designed by either making changes in an existing peptide or by designing similar molecules that functional equivalence to peptides 12 . (ijpsr.com)

Synthesis, characterization and analysis of physico-chemical properties of 1H-indol-5-yl-[4-(2-phenoxyethyl)piperazin-1-yl]methanone', Završni rad, Sveučilište u Zagrebu, Fakultet kemijskog inženjerstva i tehnologije, citirano: 25.11.2023. (unizg.hr)
Synthesis, Characterization and Electrochemistry of Open-Chain Pentapyrroles and Sapphyrins with Highly Electron Withdrawing meso-Tetraaryl substituents. (icmub.com)

The current research addresses the design, modeling, synthesis and in vitro testing of potential new DPP-IV inhibitors. (ommegaonline.org)
Ozgun, Synthesis and bioactivities of pyrazoline benzensulfonamides as carbonic anhydrase and acetylcholinesterase inhibitors with low cytotoxicity, Bioorg. (dntb.gov.ua)

Herein, we present the synthesis and antimycobacterial evaluation of a diverse set of BTZs. (ilrs.de)
Aydin, Synthesis of N-alkylated pyrazolo [3, 4-d] pyrimidine analogs and evaluation of acetylcholinesterase and carbonic anhydrase inhibition properties, Arch. (dntb.gov.ua)

Extensive in silico studies conducted indicate plasmepsin IX as a possible target for inhibitory activity of the reported molecules. (thesciencein.org)

The method that we developed allows a straightforward structural modification of bioactive molecules (e.g., α-amino acids) by the conversion of a primary amino group into a piperazine ring. (bvsalud.org)

If the destructive σ-interference effect is to benefit from the broad range of complex molecules available through modern organic synthesis, different classes of saturated systems with the effect need to be explored. (rsc.org)

It was found that the presence of saturated heterocycles from the amine molecule, 1-methyl piperazine and morpholine, respectively, contributes to an increased biological activity, compared to aromatic amino analogs, diphenylamino-, 4-nitroamino- and 4-aminobenzoic acid. (biomedcentral.com)

Find complete chemical information for 1-(METHYL-D3)PIPERAZINE 2HCL . (clearsynth.com)
1-(METHYL-D3)PIPERAZINE 2HCL in Bulk is primarily used in Pharmaceutical Industry and Drug Discovery. (clearsynth.com)
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Piperazine is one of the most frequently found scaffolds in small-molecule FDA-approved drugs. (bvsalud.org)

a ) 4,7-Dichloroquinoline design inspired by the natural molecule, chloroquine. (nature.com)
The current research aimed to design molecules maintaining the β-amino amide pharmacophore of Sitagliptin, but with the triazolo-piperazine ring system replaced by more lipophilic entities for better hydrophobic interactions with Phe 357 in the S2 pocket. (ommegaonline.org)

This unique isotopically labeled derivative of piperazine holds significant importance in various scientific and pharmaceutical applications. (clearsynth.com)

In the final step of synthesis, obtained intermediate reacted with indole-5-carboxylic acid accordingly to the Steglich mechanism of amidation using DMAP as the catalyst. (unizg.hr)
Singh, Synthesis and carbonic anhydrase inhibition studies of sulfonamide based indole-1, 2, 3-triazole chalcone hybrids, Bioorg. (dntb.gov.ua)

In addition to the ring carbons, substitution in the nitrogen atom of piperazine not only creates potential drug molecules but also makes it unique with versatile binding possibilities with metal ions. (rsc.org)
In this study, a general approach to the synthesis of piperazines bearing substituents at carbon and nitrogen atoms utilizing primary amines and nitrosoalkenes as synthons was developed. (bvsalud.org)

The Co(III) ion is six-coordinated with octahedral geometry, the pyridine rings are planar and the piperazine rings assume chair conformations. (mdpi.com)

N-dealkylation followed by hydroxylation of the piperazine ring is proposed to cause the bioactivation to iminium intermediates captured by cyanide. (bvsalud.org)
Experimental and theoretical analyses led to the identification of two key intermediates en route to DHPs and the explanation of the observed regioisomeric ratios. (ac.rs)

With regards to this result, 1H-indol-5-yl-(4-(2-phenoxyethyl)piperazine-1- yl)methanone is potentially interesting compound for further in vitro profiling of Kv1.5 inhibition. (unizg.hr)

The Erlenmeyer-Plöchl azlactone and amino acid synthesis, named after Friedrich Gustav Carl Emil Erlenmeyer who partly discovered the reaction, is a series of chemical reactions which transform an N-acyl glycine to various other amino acids via an oxazolone (also known as an azlactone). (wikipedia.org)
Furthermore, the compound's structural features contribute to its versatility in diverse chemical syntheses and analytical techniques, making it a valuable asset in the pursuit of scientific discoveries and advancements in the field of chemistry. (clearsynth.com)
Furthermore, analysis of the physico-chemical and ADME (absorption, distribution, metabolism and excretion) properties of target molecule were performed using ACDLabs/Percepta software, with aim of profiling the compound as a potential drug according to Lipinski's Ro5 rules. (unizg.hr)
Figure 3), depicts the chemical structures of the designed molecules. (ommegaonline.org)

After finishing my Ph.D. in organic chemistry, dedicated to developing new synthesis methods of polyazamacrocycles, have acquired some knowledge in spectroscopy (IR, GC-MS, NMR, Maldi-TOF, X-ray diffraction), especially in crystallography. (icmub.com)

Piperazine nucleus is found in many marketed drugs in the realm of antidepressants (amoxapine), antipsychotics (bifeprunox), antihistamines (cyclizine and oxatomide), antifungals (itraconazole), antibiotics (ciprofloxacin), etc . (rsc.org)

1,2 Consequently, even molecules with a large HOMO-LUMO gap will not be effective insulators if they are very short. (rsc.org)

In one study the Erlenmeyer amino acid synthesis was used in the heart of an L-m-tyrosine synthesis Dakin-West reaction Perkin reaction Plöchl, J. (1884). (wikipedia.org)
X-ray structure of Sitagliptin with DPP-IV indicated hydrophobic interaction of the triazolo-piperazine ring system with the S2 pocket through the amino acid Phe357. (ommegaonline.org)

The accentuated molecules could serve as a lead compound for developing 5-HT1A drug-like molecules for depression treatment. (ac.rs)

The geometry of 1-methylpiperazine, the cumulated Mullikan atomic charges of the two heteroatoms and of the methyl, and the value of the global electrophilicity index (ω = 0.0527) of the M-1 molecule is correlated with its good antimicrobial activity. (biomedcentral.com)

Straightforward synthesis of bis-tetraazacycloalkanes: towards new potential CXCR4 antagonists? (icmub.com)

X-ray crystal structure of Sitagliptin bound to DPP-IV, (Figure-2), illustrates that the triazolo-piperazine fragment of the drug is oriented towards the Phe357 residue in the catalytic site, and the trifluromethyl group towards the Ser209 residue. (ommegaonline.org)

Using the STM-BJ technique and density functional theory calculations, we confirm that their single-molecule junction conductance is lower than analogous alkanes of similar length. (rsc.org)

However, the potential has been limited to date by the restrictive structural requirements for the molecules in which the effect appears. (rsc.org)

He observed that the structure of a naturally occurring Opioid molecule: Morphine was similar to N-terminal structure of endogenous opioid peptides, Enkephalins and β-endorphin. (ijpsr.com)

TY - DATA AU - Aleksić, Jovana AU - Stojanović, Milovan AU - Bošković, Jakša AU - Baranac-Stojanović, Marija UR - http://cherry.chem.bg.ac.rs/handle/123456789/5846 AB - We present the green, highly atom-economical, solid-state silica gel-catalyzed synthesis of polysubstituted 1,4- and 1,2-dihydropyridines (DHPs) from commercially available materials, amines and ethyl propiolate. (ac.rs)
First step in synthesis included making a good leaving group from commercially available alcohol by nucleophilic substitution with mesyl-chloride. (unizg.hr)
This optimized synthesis begins with reaction of commercially available dimethyl phosphite and 2-carboxybenzaldehyde (201) to generate the corresponding phosphonate ester in 95% yield and 95% purity after aqueous workup.190 Addition of aldehyde 202 to this phosphonate ester intermediate in the presence of triethylamine led to formation of olefins 203a/203b in 96% yield as a 1:1 mixture of E/Z isomers. (chemicalbook.com)

Solid-state silica gel-catalyzed synthesis of fluorescent polysubstituted 1,4- and 1,2-dihydropyridines. (ac.rs)

In the future, drug discovery experiments utilizing this information could be performed, permitting the synthesis of new drugs with better safety profile. (bvsalud.org)

Anatomy19

Organisms14

Diseases2

Chemicals and Drugs117

Analytical, Diagnostic and Therapeutic Techniques and Equipment36

Psychiatry and Psychology3

Phenomena and Processes68

Disciplines and Occupations3

Technology, Industry, Agriculture3

Information Science3

Health Care2

Derivatives6

Compounds8

Heterocyclic5

Biological Evaluation3

Ligands3

Small molecules1

Molecular5

MOIETY2

Analogues2

Similar Molecules1

Characterization2

Inhibitors2

Evaluation2

Inhibitory activity1

Bioactive molecules1

Complex molecules1

Morpholine1

2HCL4

Scaffolds1

Design2

Derivative1

Indole2

Nitrogen2

Pyridine1

Intermediates2

Vitro1

Chemical4

Organic Chemistry1

Nucleus1

HOMO-LUMO1

Amino acid2

Compound1

Methyl1

Straightforward1

Fragment1

Density functi1

Structural1

Peptides1

Commercially available3

Fluorescent1

Drug Discovery1