新型非甾体类反向吲哚盐皮质激素受体拮抗剂的发现
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
作者信息
Ogawa Anthony K, Bunte Ellen Vande, Mal Rudrajit, Lan Ping, Sun Zhongxiang, Crespo Alejandro, Wiltsie Judyann, Clemas Joseph, Gibson Jack, Contino Lisa, Lisnock JeanMarie, Zhou Gaochao, Garcia-Calvo Margarita, Jochnowitz Nina, Ma Xiuying, Pan Yi, Brown Patricia, Zamlynny Beata, Bateman Thomas, Leung Dennis, Xu Ling, Tong Xinchun, Liu Kun, Crook Martin, Sinclair Peter
机构信息
Early Development and Discovery Sciences, Merck and Co., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
Early Development and Discovery Sciences, Merck and Co., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2016 Jun 15;26(12):2866-2869. doi: 10.1016/j.bmcl.2016.04.052. Epub 2016 Apr 20.
Reported herein are a series of reverse indoles that represent novel non-steroidal mineralocorticoid receptor (MR) antagonists. The key structure-activity relationships (SAR) are presented below. This reverse indole series is exemplified by a compound that demonstrated efficacy in an acute natriuresis rodent model comparable to marketed MR antagonists, spironolactone and eplerenone.
本文报道了一系列新型非甾体盐皮质激素受体（MR）拮抗剂——反向吲哚类化合物。以下展示了关键的构效关系（SAR）。该反向吲哚系列以一种化合物为代表，在急性利钠啮齿动物模型中显示出与市售MR拮抗剂螺内酯和依普利酮相当的疗效。
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