Search Results - "Sairam, Kalapatapu V.V.M."
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Discovery of potent, selective and orally bioavailable triaryl-sulfonamide based PTP1B inhibitors
Published in Bioorganic & medicinal chemistry letters (15-01-2012)“…A novel series of DFMP/DFMS/ISD containing triaryl-sulfonamide derivatives (5a–r) are reported as potent PTP1B inhibitors. Some of the test compounds exhibits…”
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Long-acting peptidomimetics based DPP-IV inhibitors
Published in Bioorganic & medicinal chemistry letters (15-05-2012)“…Peptidomimetic based cyanopyrrolidine derivatives are reported as potent and selective DPP-IV inhibitors. The lead compound (16c) showed long acting…”
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Synthesis and structure–activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: Application of weakly basic sulfoximine group as novel S4 binding element
Published in European journal of medicinal chemistry (01-12-2012)“…A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine moiety as novel S4 binding element in anthranilamide chemotype has…”
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Discovery of inhibitors of plasminogen activator inhibitor-1: Structure–activity study of 5-nitro-2-phenoxybenzoic acid derivatives
Published in Bioorganic & medicinal chemistry letters (01-10-2011)“…Two novel series of 5-nitro-2-phenoxybenzoic acid derivatives are designed using hybridization and conformational restriction strategy in the known chemo types…”
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Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents
Published in Bioorganic & medicinal chemistry letters (15-09-2012)“…Series of benzyl-phenoxybenzyl amino-phenyl acid derivatives are reported as non-steroidal GR antagonist. The lead compound 8g exhibited significant oral…”
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Modulation of PPAR subtype selectivity. Part 2: Transforming PPAR α/ γ dual agonist into α selective PPAR agonist through bioisosteric modification
Published in Bioorganic & medicinal chemistry letters (15-01-2011)“…A novel series of oxime containing benzyl-1,3-dioxane- r-2-carboxylic acid derivatives are reported as selective PPAR α agonists. Some of the test compounds…”
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Peptidomimetics as potent and selective PTP1B inhibitors
Published in Medicinal chemistry (Shp-sariqah, United Arab Emirates) (01-08-2013)“…A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed…”
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Three Dimensional Pharmacophore Modelling of Monoamine oxidase-A (MAO-A) inhibitors
Published in International journal of molecular sciences (01-09-2007)“…Flavoprotein monoamine oxidase is located on the outer membrane ofmitochondria. It catalyzes oxidative deamination of monoamine neurotransmitters such…”
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In the Quest for Potent and Selective Malic Enzyme 3 Inhibitors for the Treatment of Pancreatic Ductal Adenocarcinoma
Published in ACS medicinal chemistry letters (12-01-2023)“…The genome of pancreatic ductal adenocarcinoma (PDAC) is associated with frequent deletion of the tumor suppressor gene SMAD family member 4 (SMAD4) with…”
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Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors
Published in Bioorganic & medicinal chemistry letters (15-04-2014)“…A series of novel aminomethyl-piperidones were designed and evaluated as potential DPP-IV inhibitors. Optimized analogue 12v…”
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11
Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist
Published in ACS medicinal chemistry letters (14-01-2016)“…TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. The…”
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Discovery of Orally Active, Potent, and Selective Benzotriazole-Based PTP1B Inhibitors
Published in ChemMedChem (06-06-2011)“…A two‐hand grasp on one enzyme: A novel series of dual‐site benzotriazole derivatives are reported as potent PTP1B inhibitors. Some of the test compounds…”
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13
Modulation of PPAR receptor subtype selectivity of the ligands: Aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety
Published in Bioorganic & medicinal chemistry (15-12-2008)“…Oxazole containing glycine and oximinobutyric acid derivatives were synthesized as PPARα agonists by incorporating polymethylene spacer as a replacement of…”
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Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist
Published in Bioorganic & medicinal chemistry letters (15-07-2008)“…Facile synthesis of biaryl pyrazole sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid…”
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Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
Published in Bioorganic & medicinal chemistry letters (01-02-2008)“…Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of…”
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Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1 H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist
Published in Bioorganic & medicinal chemistry letters (2008)“…Facile synthesis of biaryl pyrazole sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1 H-pyrazole-3-carboxylic acid…”
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17
Bioisosteric replacement of dihydropyrazole of 4 S-(−)-3-(4-chlorophenyl)- N-methyl- N′-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
Published in Bioorganic & medicinal chemistry letters (2008)“…Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of 4 S-(−)-3-(4-chlorophenyl)- N-methyl-…”
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18
3D-QSAR studies of some [[1-aryl(or benzyl)-1-(benzenesulphonamido)methyl] phenyl] alkanoic acid derivatives as thromboxane A2 receptor antagonists
Published in Drug design and discovery (2003)“…Thromboxane A(2) receptor antagonists have attracted much attention in recent times in the design of new agents that could be active against diseases such as…”
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