Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists

作者：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

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(15): 4388-4392.

DOI：10.1016/j.bmcl.2013.05.077

• Mineralocorticoid receptor antagonist
• Hypertension

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 demonstrated excellent MR activity, reasonable nuclear hormone receptor selectivity, and acceptable rat pharmacokinetics.

• 出版日期2013-8-1