具有乙酰胺基团的环磺酰胺衍生物作为11β-羟基类固醇脱氢酶1抑制剂的鉴定。
Identification of cyclicsulfonamide derivatives with an acetamide group as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
作者信息
Kim Se Hoan, Kwon Sung Wook, Chu So Young, Lee Jae Hong, Narsaiah Banda, Kim Chi Hyun, Kang Seung Kyu, Kang Nam Sook, Rhee Sang Dal, Bae Myung Ae, Ahn Sung Hoon, Ha Duck Chan, Kim Ki Young, Ahn Jin Hee
机构信息
Department of Chemistry, Korea University, Seoul, Korea.
出版信息
Chem Pharm Bull (Tokyo). 2011;59(1):46-52. doi: 10.1248/cpb.59.46.
In the continuation of our 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor research, cyclic sulfonamide derivatives with an acetamide group at the 2-position were synthesized and evaluated for their abilities to inhibit 11β-HSD1. Among this series, Compound 34 showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-HSD2, microsomal stability, good pharmacokinetic and safety profiles human ether-a-go-go related gene (hERG and cytochrome P450 (CYP)). Also, a docking study explained the activity difference between human and mouse 11β-HSD1.
在我们对11β-羟基类固醇脱氢酶1型（11β-HSD1）抑制剂的持续研究中，合成了在2-位带有乙酰胺基的环状磺酰胺衍生物，并评估了它们抑制11β-HSD1的能力。在该系列化合物中，化合物34对人11β-HSD1表现出良好的体外活性、对11β-HSD2的选择性、微粒体稳定性、良好的药代动力学和安全性，以及对人醚-去极化相关基因（hERG）和细胞色素P450（CYP）的安全性。此外，一项对接研究解释了人和小鼠11β-HSD1之间的活性差异。
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