Resurrecting the Condemned: Identification of N-Benzoxaborole Benzofuran GSK8175 as a Clinical Candidate with Reduced Metabolic Liability.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00415
Abstract: Recently, in a program designed to improve the metabolic stability of the HCV inhibitor GSK5852, N-benzoxaborole benzofuran (GSK8175) emerged as a clinical candidate that not only retains the broad-spectrum activity against HCV subgenomic replicons but… read more here.
Keywords: benzoxaborole benzofuran; chemistry; clinical candidate; benzofuran gsk8175 ... See more keywords
Mitigating the Metabolic Liability of Carbonyl Reduction: Novel Calpain Inhibitors with P1' Extension.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.7b00494
Abstract: Dysregulation of calpains 1 and 2 has been implicated in a variety of pathological disorders including ischemia/reperfusion injuries, kidney diseases, cataract formation, and neurodegenerative diseases such as Alzheimer's disease (AD). 2-(3-Phenyl-1H)-pyrazol-1-yl)nicotinamides represent a series of… read more here.
Keywords: novel; calpain inhibitors; metabolic liability; carbonyl reduction ... See more keywords