AEGiS-PRn: Hughes Institute: Scientists Develop Potent New Inhibitors of the AIDS Virus PRNewswireImportant note: Information in this article was accurate in 1998. The state of the art may have changed since the publication date.
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Hughes Institute: Scientists Develop Potent New Inhibitors of the AIDS Virus

PR Newswire; Friday July 10, 10:26 am EST


ST. PAUL, Minn., July 10 /PRNewswire/ -- In an exciting new discovery scientists at the Hughes Institute have developed potent new inhibitors of the AIDS virus. Designated as S-DABO compounds, these novel drugs prevent the spread of HIV into healthy cells and stop HIV from growing inside the elements of the immune system. More specifically, the drugs paralyze the enzyme critical for the growth of the AIDS virus, known as reverse transcriptase (RT). This new breakthrough in the fight against AIDS is likely to stimulate new research since it describes how powerful anti-AIDS drugs can be prepared by taking advantage of a novel computer model anticipated to significantly facilitate drug discovery efforts against AIDS.

The new anti-AIDS drugs reported by Hughes Institute scientists were developed by applying state-of-the-art methods and tools from multiple scientific disciplines, including physics, mathematics, and chemistry to a rational drug design against the AIDS virus. The lead compound elicited potent anti-HIV activity and completely inhibited the replication of the AIDS virus in human lymphocytes. The treatment was not associated with any toxicity to human lymphocytes.

Hughes Institute scientists are now in a position to make many more potent anti-AIDS drugs using a computer model they established to predict with a degree of accuracy which drugs would be effective against the AIDS virus. The description of the design and synthesis of the potent anti-HIV drugs as well as the novel computer model for rational drug design against AIDS are being reported in this month's issue of the prestigious drug discovery and chemistry journal, Bioorganic & Medicinal Chemistry Letters.

Reference: Vig R, Mao C, Venkatachalam TK, Tuel-Ahlgren L, Sudbeck EA, Uckun FM. 5-Alkyl-2-((methylthiomethyl)thio)-6-(benzyl)-pyridmidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series. Bioorganic & Medicinal Chemistry Letters, 8(12):1461-1466, 1998.

SOURCE: Hughes Institute


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