发现新型恶唑烷二酮衍生物作为有效和选择性的盐皮质激素受体拮抗剂。
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
机构信息
Department of Discovery Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
出版信息
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4388-92. doi: 10.1016/j.bmcl.2013.05.077. Epub 2013 Jun 4.
PMID:23777778
Abstract
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.
摘要
新型恶唑烷二酮类似物被发现是具有强效和选择性的盐皮质激素受体 (MR) 拮抗剂。构效关系 (SAR) 研究集中于提高化合物的效力和微粒体稳定性。部分化合物表现出优异的 MR 活性、合理的核激素受体选择性和可接受的大鼠药代动力学特性。
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