Inhibitors of HIV protease: unique non-peptide active site templates. NLM AIDSLINE Important note: Information in this article was accurate in 1997. The state of the art may have changed since the publication date.

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Inhibitors of HIV protease: unique non-peptide active site templates.

J Mol Recognit. 1996 Mar-Apr;9(2):139-42. Unique Identifier : AIDSLINE MED/97031899
Tait BD; Domagala J; Ellsworth EL; Ferguson D; Gajda C; Hupe D; Lunney EA; Tummino PJ; Department of Chemistry, Parke-Davis Pharmaceutical Research Division; of the Warner-Lambert Company, Ann Arbor, Michigan 48106, USA.

Abstract: New templates were designed and prepared which straddle the active site of HIV-1 protease. These templates were designed to be "flexible scaffolds' upon which substituents could be appended to fill the pockets of HIV protease. The new templates prepared and analysed were 4-hydroxy-5H-furan-2-ones, 4-hydroxy-5,6-dihydropyrones, 3-hydroxy-cyclohex-2-enones, and 4-hydroxy-2(1H)-pyridinones, of which the 4-hydroxy-5,6-dihydropyrones were found to be the most potent inhibitors of HIV-1 protease.
Keywords: *HIV Protease/METABOLISM *HIV Protease Inhibitors/CHEMISTRY *HIV Protease Inhibitors/METABOLISMKWDhivprotease/metabolismKWDhivproteaseinhibitors/chemistryKWDhivproteaseinhibitors/metabolism
970430
M9741605

Copyright © 1997 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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