Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro

被引：35
|
作者：
Ran, Jun-Qiang [1 ]
Huang, Ning [2 ]
Xu, Hui [1 ]
Yang, Liu-Meng [2 ]
Lv, Min [1 ]
Zheng, Yong-Tang [2 ]
机构：
[1] NW A&F Univ, Coll Sci, Lab Pharmaceut Design & Synth, Yangling 712100, Peoples R China
[2] Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech Chinese Acad, Kunming 650223, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 12期
关键词：
N-Arylsulfonyl-3-acetylindole; Acquired immune-deficiency syndrome; Human immunodeficiency virus-1; Inhibitor;
D O I：
10.1016/j.bmcl.2010.04.132
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC50 values of 0.36 and 0.13 mu g/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3534 / 3536
页数：3
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