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Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R1-R7, X, X’, Y, Y’, Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5055N – PubChem

 

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In this study azetidine derivatives representing conformationally constrained GABA or beta-alanine analogs were evaluated for their potency as GABA-uptake inhibitors. The study comprised derivatives substituted in 2- as well as in 3-position with either an acetic acid moiety or a carboxylic acid function. In addition, azetidine derivatives bearing a tetrazole ring as a bioisosteric substitute for a carboxylic acid group were included. 3-Hydroxy-3-(4-methoxyphenyl)azetidine derivatives were explored as analogs of the known GABA-uptake inhibitor NNC-05-2045 exhibiting an azetidine ring instead of a piperidine ring present in the latter. Both, N-unsubstituted compounds as well as their N-alkylated lipophilic derivatives, were biologically evaluated for their affinity to the GAT-1 and GAT-3 transporters. Azetidin-2-ylacetic acid derivatives provided with a 4,4-diphenylbutenyl or 4,4-bis(3-methyl-2-thienyl)butenyl moiety as lipophilic residue were found to exhibit the highest potency at GAT-1 with IC50 values of 2.83 ± 0.67 muM and 2.01 ± 0.77 muM, respectively. The most potent GAT-3 inhibitor among these compounds appeared to be the beta-alanine analog 1-{2-[tris(4-methoxyphenyl)methoxy]ethyl}azetidine-3-carboxylic acid (12d) displaying an IC50 value of 15.3 ± 4.5 muM. Whereas the tetrazole derivatives showed no potency as GABA-uptake inhibitors, the 3-hydroxy-3-(4-methoxyphenyl)azetidine derivatives exhibited moderate affinity to GAT-1 (compound 18b: IC50 = 26.6 ± 3.3 muM) and to GAT-3 (compound 18e: IC50 = 31.0 ± 4.7 muM).

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5036N – PubChem

 

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Related Products of 25137-00-2, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 25137-00-2, Name is (R)-Piperidine-3-carboxylic acid, molecular formula is C6H11NO2. In a Article,once mentioned of 25137-00-2

We examine the relationship between covalent structure and conformational propensity among a series of beta-amino acid tetramers. These experiments focus on the hairpin folding motif. Among conventional peptides, the minimum increment of beta-sheet secondary structure is a ‘beta-hairpin,’ in which two strands are connected via a short loop. The present studies are aimed at optimizing hairpin stability among beta-peptides. Previous work from our laboratory has identified optimal substitution patterns for residues that form strands in an antiparallel beta-peptide sheet (Krauthauser et al. J. Am. Chem. Soc. 1997, 119, 11719), and we have shown that a dinipecotic acid segment can promote sheet-type interactions between attached strand residues (Chung et al. J. Am. Chem. Soc. 1998, 120, 10555). Here we compare all four possible configurations of the dinipecotic acid segment, (R,S), (S,R), (R,R) and (S,S), for the ability to induce sheet formation with a constant set of enantiomerically pure strand residues. We show that both heterochiral dinipecotic acid segments promote hairpin formation, although one is distinctly superior. Neither of the homochiral dinipecotic acid supports hairpin folding. When the strand residues are beta-alanine (achiral), the heterochiral dinipecotic acid segment is again superior to the homochiral segment, but we find a difference between hairpin conformations in solution and in the solid state.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5003N – PubChem

 

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Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about is helpful to your research. category: piperidines

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, category: piperidines, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 25137-00-2, Name is (R)-Piperidine-3-carboxylic acid, molecular formula is C6H11NO2. In a Patent, authors is ,once mentioned of 25137-00-2

The present application relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables are’as defined in the claims. The present application also relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome in an affected mammal by administering a compound of formula (I) or a pharmaceutically acceptable salt thereof.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5016N – PubChem

 

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A series of PI3Kdelta inhibitors derived from the pan-PI3K inhibitor ZSTK474 was prepared that target a non-conserved region of the catalytic site. Dependent upon the substituents present, these analogues show different levels of isoform selectivity and sensitivity to the mutation N836D in PI3Kdelta. As a marker of ?on-target? activity and permeability, a selection of the most potent PI3Kdelta inhibitors were shown to inhibit pAkt production in the Nawalma Burkitt lymphoma cell line.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5062N – PubChem

 

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 25137-00-2, molcular formula is C6H11NO2, introducing its new discovery. Safety of (R)-Piperidine-3-carboxylic acid

Direct inhibition of coagulation factor Xa (FXa) carries significant promise for developing effective and safe anticoagulants. Although a large number of FXa inhibitors have been studied, each can be classified as either possessing a highly flexible or a rigid core scaffold. We reasoned that an intermediate level of flexibility will provide high selectivity for FXa considering that its active site is less constrained in comparison to thrombin and more constrained as compared to trypsin. We studied several core scaffolds including 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid for direct FXa inhibition. Using a genetic algorithm-based docking and scoring approach, a promising candidate 23 was identified, synthesized, and found to inhibit FXa with a Ki of 28 muM. Optimization of derivative 23 resulted in the design of a potent dicarboxamide 47, which displayed a Ki of 135 nM. Dicarboxamide 47 displayed at least 1852-fold selectivity for FXa inhibition over other coagulation enzymes and doubled PT and aPTT of human plasma at 17.1 muM and 20.2 muM, respectively, which are comparable to those of clinically relevant agents. Dicarboxamide 47 is expected to serve as an excellent lead for further anticoagulant discovery.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5049N – PubChem

 

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Central nervous system (CNS) selective amino acid transporters provide an important function in maintaining tonic extracellular levels of amino acids that act as neurotransmitters synaptic modulators or neurotransmitter precursors. Small molecule inhibitors of these transporters have been postulated and in some cases demonstrated to be useful in the treatment of a range of CNS driven disorders such as epilepsy, anxiety, psychosis, depression, pain and neurodegenerative disease. Although much of the research to date in this field has focussed on inhibition of the gamma-amino butyric acid (GABA) transporters more recent reports have also generated interest in modulation of glycine, glutamate and proline transporters. This article will review the current medicinal chemistry literature and structure activity relationships known for mammalian CNS selective amino acid transporters.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5056N – PubChem

 

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Docking and pharmacodynamic studies on hGAT1 inhibition activity in the presence of selected neuronal and astrocytic inhibitors. Part I

Inhibition of 4-aminobutanoic acid (GABA) uptake is a strategy for enhancing GABA transmission. The utility of this approach is demonstrated by the successful development of such agents for the treatment of epilepsy and pain. Existing reports on acute brain slice preparations indicate the intersecting of complementary channels and receptors sets between astrocytes and neurons cells. Thorough analysis of astroglial cells by means of molecular and functional studies demonstrated their active modulatory role in intercellular communication. The chemical interactions between sixteen GABA analogues and isoform of hGAT1 is outlined in the light of molecular docking results. In the in vivo part antinociceptive properties of racemic nipecotic acid, its R and S enantiomers and isonipecotic acid, each administered intraperitoneally at 3 fixed doses (10, 30 and 100 mg/kg), were assessed in a thermally-induced acute pain model i.e. the mouse hot plate test. Docking analyses provided complex binding energies, specific h-bond components, and h-bond properties, such as energies, distances and angles. In vivo tests revealed statistically significant antinociceptive properties of isonipecotic acid (10 and 30 mg/kg), R-nipecotic acid (30 and 100 mg/kg) and S-nipecotic acid (100 mg/kg) in mice. The docking data endorse the hypothesis of correlation between the strength of their chemical interactions with hGAT1 and analgesic action of studied compounds.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H5034N – PubChem

 

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Orally active and potent inhibitors of gamma-aminobutyric acid uptake

3-Pyrrolidineacetic acid (1a), certain piperidinecarboxylic acids – i.e., 3-piperidinecarboxylic acid (2a), 1,2,5,6-tetrahydro-3-pyridinecarboxylic acid (3a), and cis-4-hydroxy-3-piperidinecarboxylic acid (4a) – cis-3-aminocyclohexanecarboxylic acid (5a, cis-3-ACHC), and gamma-aminobutyric acid (6a, GABA) itself are among the most potent inhibitors of [3H]GABA uptake by neurons and glia in vitro. These hydrophilic amino acids, however, do not readily enter the central nervous system in pharmacologically significant amounts following peripheral administration. We now report that N-(4,4-diphenyl-3-butenyl)-3-piperidinecarboxylic acid is a specific GABA-uptake inhibitor that is more potent, more lipophilic and, in limited testing, as selective as 2a. Similar results were obtained with the N-(4,4-diphenyl-3-butenyl) derivatives of 1a, 3a, and 4a. By contrast, N-(4,4-diphenyl-3-butenyl) derivatives of 5a and 6a were not more potent than the parent amino acids and appear to inhibit GABA uptake, at least in part, by a nonselective mechanism of action. The N-(4,4-diphenyl-3-butenyl)amino acids exhibit anticonvulsant activity in rodents following oral or intraperitoneal administration.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H5082N – PubChem

 

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A parallel preparation of a bicyclic N-chiral amine library and its use for chiral catalyst screening

A parallel library of optically active bicyclic tertiary amines bearing N-chiral bridgehead nitrogen atoms was readily prepared by condensation of primary amines, cyclic amino acids and aldehydes. The enantiocontrolling ability of each of the library members was examined for the asymmetric alkylation of benzaldehyde with diethylzinc, and (3R,6R,7aS)-(2,3-diphenyl-6-hydroxy)hexahydro-1H-pyrrolo[1,2-c]imidazol-1- one, which contains a beta-amino alcohol unit, showed high enantioselectivity.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H5071N – PubChem