非肽类HIV蛋白酶抑制剂：基于C2对称性的双磺酰胺二氢吡喃酮设计
Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones.
作者信息
Janakiraman M N, Watenpaugh K D, Tomich P K, Chong K T, Turner S R, Tommasi R A, Thaisrivongs S, Strohbach J W
机构信息
Pharmacia & Upjohn, Inc., Kalamazoo, Michigan 49001, USA.
出版信息
Bioorg Med Chem Lett. 1998 May 19;8(10):1237-42. doi: 10.1016/s0960-894x(98)00197-8.
PMID:9871742
Abstract
Potent, non-peptidic, dihydropyrone sulfonamide HIV protease inhibitors have been previously described. Crystallographic analysis of dihydropyrone sulfonamide inhibitor/HIV protease complexes suggested incorporation of a second, C2 symmetry-related sulfonamide group. Selected bis-sulfonamide dihydropyrone analogues display high HIV protease inhibitory activity.
摘要
强效、非肽类二氢吡喃磺酰胺HIV蛋白酶抑制剂此前已有报道。二氢吡喃磺酰胺抑制剂/HIV蛋白酶复合物的晶体学分析表明引入了第二个与C2对称相关的磺酰胺基团。选定的双磺酰胺二氢吡喃类似物显示出高HIV蛋白酶抑制活性。
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