title: Anti HIV-1 agents 6. Synthesis and anti-HIV-1 activity of indolyl glyoxamides.
abstract: In order to discover compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 9 new indolyl glyoxamide derivatives (3a-i) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among all the derivatives, especially compounds 3e and 3h showed the potent anti-HIV-1 activity with EC(50) values of 6.83 and 4.35 µg/mL, and TI values of >27.15 and 49.45, respectively. It demonstrated that introduction of the substituent R(3) as the halogen atom and the position of R(3) were generally important to their activity.
authors: Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, PR China.
authors: Yi
authors: Y
authors: Wang
authors: Ning
authors: N
authors: Huang
authors: Xiang
authors: X
authors: Yu
authors: Liu-Meng
authors: LM
authors: Yang
authors: Xiao-Yan
authors: XY
authors: Zhi
authors: Yong-Tang
authors: YT
authors: Zheng
authors: Hui
authors: H
authors: Xu
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D016333:HIV Protease / Q000737:chemistry* / Q000378:metabolism; D017320:HIV Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006219:Halogens / Q000737:chemistry; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013453:Sulfonylurea Compounds / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D006219:Halogens; D007211:Indoles; D013453:Sulfonylurea Compounds; D016333:HIV Protease