Discovery of Benzimidazole Oxazolidinediones as Novel and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists
作者:Christine Yang、Jaume Balsells、Hong D. Chu、Jason M. Cox、Alejandro Crespo、Xiuying Ma、Lisa Contino、Patricia Brown、Sheng Gao、Beata Zamlynny、Judyann Wiltsie、Joseph Clemas、JeanMarie Lisnock、Jack Gibson、Gaochao Zhou、Margarita Garcia-Calvo、Thomas J. Bateman、Vincent Tong、Ling Xu、Martin Crook、Peter Sinclair、Hong C. Shen
DOI:10.1021/acsmedchemlett.5b00010
日期:2015.4.9
Elaboration of the oxazolidinedione series led to replacement of the exocyclic amides with substituted benzimidazoles. The structure-activity relationship (SAR) exploration resulted in the discovery of potent and selective nonsteroidal mineralocorticoid receptor (MR) antagonists with significantly improved microsomal stability and pharmacokinetic (PK) profile relative to the HTS hit 1a. One compound
[EN] PROTECTIVE TAPE, SEMICONDUCTOR PROTECTIVE TAPE, AND METHOD FOR PRODUCING SEMICONDUCTOR DEVICE<br/>[FR] BANDE DE PROTECTION, BANDE DE PROTECTION DE SEMI-CONDUCTEUR ET PROCÉDÉ DE PRODUCTION DE DISPOSITIF À SEMI-CONDUCTEUR<br/>[JA] 保護テープ、半導体保護テープ及び半導体デバイスの製造方法
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1
作者:Mohamed Benchekroun、Ludmila Ermolenko、Minh Quan Tran、Agathe Vagneux、Hristo Nedev、Claire Delehouzé、Mohamed Souab、Blandine Baratte、Béatrice Josselin、Bogdan I. Iorga、Sandrine Ruchaud、Stéphane Bach、Ali Al-Mourabit
DOI:10.1016/j.ejmech.2020.112337
日期:2020.9
tools based on simplified natural metabolites to help deciphering the molecular mechanism of necroptosis, simplified benzazole fragments including 2-aminobenzimidazole and the 2-aminobenzothiazole analogs were prepared during the synthesis of the marine benzosceptrin B. Conpounds inhibiting the RIPK1 proteinkinase were discovered. A library of 54 synthetic analogues were prepared and evaluated through