Vijay Keshav Gore

TL;DR: This review details developments of new, highly atom-economic MCR derived chemical methods, which enable the fast and efficient production of chemical libraries comprised of a variety of biologically relevant templates, and focuses on applications of isocyanide based MCR (IMCR) reactions.

TL;DR: The synthesis and the structure-activity relationships of a series of 2-(4-pyridin-2-ylpiperazin-1-yl)-1H-benzo[d]imidazoles as novel TRPV1 antagonists are described and compound 46ad was among the most potent analogues in this series.

TL;DR: Based on its improved overall profile, compound 16p (AMG 628) was selected as a second-generation candidate for further evaluation in human clinical trials as a potential new treatment for chronic pain.

TL;DR: In this paper, a further application of N -BOC-α-aminoaldehydes in the Ugi condensation reaction, followed by a secondary S N Ar cyclization, accessing arrays of biologically relevant benzodiazepines in good yield and overall purity.

TL;DR: Exploration of the structure-activity relationships of 4 led to the identification of a potent and orally bioavailable TRPM8 antagonist, tetrahydroisoquinoline 87, which demonstrated target coverage in vivo after oral administration in a rat pharmacodynamic model measuring the prevention of icilin-induced wet-dog shakes (WDS).