HIV-1 protease inhibitory activity of L-694,746, a novel metabolite of L-689,502

  • Biochem Biophys Res Commun. 1991 Dec 31;181(3):1456-61. doi: 10.1016/0006-291x(91)92103-q.
R B Lingham  1 ,  B H Arison ,  L F Colwell ,  A Hsu ,  G Dezeny ,  W J Thompson ,  G M Garrity ,  M M Gagliardi ,  F W Hartner ,  P L Darke, et al.
Affiliations
  • 1. Merck, Sharp and Dohme Research Laboratories, Rahway, New Jersey 07065.
PMID: 1764098 DOI: 10.1016/0006-291x(91)92103-q
Abstract

L-689,502 is a potent inhibitor of HIV-1 protease activity in vitro. Microbial biotransformations of L-689,502 by cultures belonging to the genus Streptomyces sp. were performed. Extracts of culture broths were examined for the production of metabolites of L-689,502 that could inhibit HIV-1 protease activity. One culture, MA 6804 (Streptomyces lavendulae, ATCC 55095), produced L-694,746 that, while being structurally related to L-689,502, is a novel metabolite and a potent inhibitor of HIV-1 protease.

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