Article
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.
Journal of medicinal chemistry - 14 Jul 2011
Chung Suhman, Himmel Daniel M, Jiang Jian-Kang, Wojtak Krzysztof, Bauman Joseph D, Rausch Jason W, Wilson Jennifer A, Beutler John A, Thomas Craig J, Arnold Eddy, Le Grice Stuart F J
Abstract excerpt
The α-hydroxytroplone, manicol (5,7-dihydroxy-2-isopropenyl-9-methyl-1,2,3,4-tetrahydro-benzocyclohepten-6-one), potently and specifically inhibits ribonuclease H (RNase H) activity of human immunodeficiency virus reverse transcriptase (HIV RT) in vitro. However, manicol was ineffective in reducing virus replication in culture. Ongoing efforts to improve the potency and specificity over the lead compound led us...
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