作为HIV-1逆转录酶非核苷抑制剂的三唑衍生物——构效关系及晶体学分析
Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis.
作者信息
Kirschberg Thorsten A, Balakrishnan Mini, Huang Wei, Hluhanich Rebecca, Kutty Nilima, Liclican Albert C, McColl Damian J, Squires Neil H, Lansdon Eric B
机构信息
Gilead Sciences, Department of Medicinal Chemistry, 333 Lakeside Drive, Foster City, CA 94404, USA.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1131-4. doi: 10.1016/j.bmcl.2007.11.127. Epub 2007 Dec 5.
PMID:18083512
Abstract
A series of 3,4,5-trisubstituted 1,2,4-4H triazole derivatives was synthesized and investigated for HIV-1 reverse transcriptase inhibition. An X-ray structure with HIV-1 RT secured the binding mode and allowed the key interactions with the enzyme to be identified.
摘要
合成了一系列3,4,5-三取代的1,2,4-4H三唑衍生物，并对其抑制HIV-1逆转录酶的活性进行了研究。HIV-1逆转录酶的X射线晶体结构确定了其结合模式，并使与该酶的关键相互作用得以确定。
Zotero 插件