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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.

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  • Authors

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

    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