Search Results - "BRIJESH KUMAR SRIVASTAVA"
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Discovery of novel, potent and orally efficacious inhibitor of neutral amino acid transporter B0AT1 (SLC6A19)
Published in Bioorganic & medicinal chemistry letters (01-12-2021)“…[Display omitted] •Inhibition of neutral amino acid transporter B0AT1 (SLC6A19) activity has been recently identified as promising strategy to treat type 2…”
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Diaryl Dihydropyrazole-3-carboxamides with Significant In Vivo Antiobesity Activity Related to CB1 Receptor Antagonism: Synthesis, Biological Evaluation, and Molecular Modeling in the Homology Model
Published in Journal of medicinal chemistry (29-11-2007)“…A number of analogues of diaryl dihydropyrazole-3-carboxamides have been synthesized. Their activities were evaluated for appetite suppression and body weight…”
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Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2- c]pyridine quinolones
Published in Bioorganic & medicinal chemistry letters (01-04-2007)“…Synthesis and antibacterial activity of a number of substituted 4,5,6,7-tetrahydro-thieno[3,2- c]pyridine quinolones is reported. The antibacterial activities…”
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3D QSAR studies of N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones: A novel class of antibacterial agents
Published in Bioorganic & medicinal chemistry letters (15-07-2006)“…Three-dimensional QSAR studies for N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones were conducted using TSAR 3.3. The in vitro activities (MICs) of the…”
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Synthesis and in vitro antibacterial activities of novel oxazolidinones
Published in European journal of medicinal chemistry (01-04-2008)“…Design and synthesis of novel piperazinylaryloxazolidinones possessing heteroaryl groups are described and their in vitro antibacterial activities have been…”
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Novel tetrahydro-thieno pyridyl oxazolidinone: an antibacterial agent
Published in Bioorganic & medicinal chemistry (01-09-2004)“…We have synthesized and evaluated antibacterial activity of a number of 4,5,6,7-tetrahydro-thieno[3,2- c]pyridine substituted oxazolidinones against several…”
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Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials
Published in Bioorganic & medicinal chemistry letters (15-03-2006)“…A few substituted piperazinylphenyloxazolidinone compounds 6–13 having substitution on the distant nitrogen atom of piperazine ring scaffold have been…”
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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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9
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones
Published in Bioorganic & medicinal chemistry letters (15-09-2007)“…Design and synthesis of a few novel methylamino piperidinyl substituted oxazolidinones are reported and their antibacterial activities have been evaluated in…”
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10
Oxazolidinone: search for highly potent antibacterial
Published in Bioorganic & medicinal chemistry letters (21-06-2004)“…A number of substituted piperazinyl oxazolidinone derivatives have been synthesized and their antibacterial activities were evaluated. A systematic SAR was…”
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11
Novel Mannich ketones of oxazolidinones as antibacterial agents
Published in European journal of medicinal chemistry (01-11-2004)“…A few Mannich ketones of piperazinyl oxazolidinone derivatives have been synthesized and their antibacterial activity in various Gram-positive organisms such…”
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ZYDG2, a Potent, Selective, and Safe GPR40 Agonist for Treatment of Type 2 Diabetes
Published in Diabetes (New York, N.Y.) (01-07-2018)“…GPR40 is a G-protein-coupled receptor predominantly expressed in pancreatic β-cells. Agonists of GPR40 are known to stimulate insulin secretion and reduces…”
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Identification and preclinical characterization of a novel and potent poly (ADP-ribose) polymerase (PARP) inhibitor ZYTP1
Published in Cancer chemotherapy and pharmacology (01-10-2018)“…Purpose Poly(ADP-ribose) polymerase-1 (PARP-1) is a nuclear enzyme involved in the detection and repair of DNA damage. Studies have shown that inhibition of…”
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Cannabinoid receptor 1 antagonist treatment induces glucagon release and shows an additive therapeutic effect with GLP-1 agonist in diet-induced obese mice
Published in Canadian journal of physiology and pharmacology (01-12-2014)“…Cannabinoid 1 (CB1) receptor antagonists reduce body weight and improve insulin sensitivity. Preclinical data indicates that an acute dose of CB1 antagonist…”
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Discovery of novel, potent and orally efficacious inhibitor of neutral amino acid transporter B 0 AT1 (SLC6A19)
Published in Bioorganic & medicinal chemistry letters (01-12-2021)“…Amino acid restriction by inhibition of neutral amino acid transporter, B AT1 (SLC6A19) activity has been recently shown to improve glyceamic control by…”
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16
Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect
Published in Bioorganic & medicinal chemistry letters (01-05-2009)“…A few thienyl substituted pyrazole derivatives were synthesized to aid in the characterization of the cannabinoid receptor antagonist and also to serve as…”
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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)-l-(2.4-dichlorophenyl)-4-methyl-lH-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist
Published in Bioorganic & medicinal chemistry letters (2008)Get full text
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20
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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