Santosh Sasane
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View article: Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor
Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor Open
View article: CCDC 1840518: Experimental Crystal Structure Determination
CCDC 1840518: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Discovery of <i>N</i>-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors
Discovery of <i>N</i>-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors Open
NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases. In this study, rationally designed mimics of sulfonylurea moiety were investigated as NLRP3 inhibitors. Our results culminated into disc…
View article: Novel 2-mercapto imidazole and triazole derivatives as potent TGR5 receptor agonists
Novel 2-mercapto imidazole and triazole derivatives as potent TGR5 receptor agonists Open
TGR5 is a bile acid G protein-coupled receptor (GPCR), which is an attractive therapeutic target for the treatment of obesity, and its highly associated Type 2 diabetes. Activation of TGR5 promotes secretion of glucagon like peptide-1 (GLP…
View article: Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes
Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes Open
View article: Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist
Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist Open
GPR40/FFAR1 is a G protein-coupled receptor predominantly expressed in pancreatic β-cells and activated by long-chain free fatty acids, mediating enhancement of glucose-stimulated insulin secretion. A novel series of substituted 3-(4-arylo…
View article: Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist
Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist Open
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 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR…