1430104-90-7Relevant articles and documents
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists
Yang, Christine,Balsells, Jaume,Chu, Hong D.,Cox, Jason M.,Crespo, Alejandro,Ma, Xiuying,Contino, Lisa,Brown, Patricia,Gao, Sheng,Zamlynny, Beata,Wiltsie, Judyann,Clemas, Joseph,Lisnock, Jeanmarie,Gibson, Jack,Zhou, Gaochao,Garcia-Calvo, Margarita,Bateman, Thomas J.,Tong, Vincent,Xu, Ling,Crook, Martin,Sinclair, Peter,Shen, Hong C.
, p. 461 - 465 (2015/04/27)
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 2p possessed comparable efficacy as spironolactone (SPL) at 100 mg/kg (p.o.) in the rat natriuresis model. As such, this series was validated as a lead series for further optimization.
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists
Yang, Christine,Shen, Hong C.,Wu, Zhicai,Chu, Hong D.,Cox, Jason M.,Balsells, Jaume,Crespo, Alejandro,Brown, Patricia,Zamlynny, Beata,Wiltsie, Judyann,Clemas, Joseph,Gibson, Jack,Contino, Lisa,Lisnock, Jeanmarie,Zhou, Gaochao,Garcia-Calvo, Margarita,Bateman, Tom,Xu, Ling,Tong, Xinchun,Crook, Martin,Sinclair, Peter
, p. 4388 - 4392 (2013/07/26)
Novel oxazolidinedione analogs were discovered as potent and selective mineralocorticoid receptor (MR) antagonists. Structure-activity relationship (SAR) studies were focused on improving the potency and microsomal stability. Selected compounds demonstrat
