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.

Links

Publisher Full Text

Authors

Wang Y, Huang N, Yu X, Yang LM, Zhi XY, Zheng YT, Xu H

Institution

Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, PR China.

Source

Medicinal chemistry (Shāriqah (United Arab Emirates)) 8:5 2012 Sep pg 831-3

MeSH

Anti-HIV Agents
Cell Line
HIV Protease
HIV Protease Inhibitors
HIV-1
Halogens
Humans
Indoles
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Molecular Structure
Structure-Activity Relationship
Sulfonylurea Compounds

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22741604