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Chemical Compound Review

CHEMBL83622     3-(2-benzooxazol-2-ylethyl)- 5-ethyl-6...

Synonyms: AG-J-85056, SureCN5573693, ACMC-20mvsk, AC1L2HWM, CTK0H7281, ...
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Disease relevance of AIDS003337


High impact information on AIDS003337

  • L-702,019 was also a potent inhibitor of the replication of mutant HIV-1 containing the individual mutations at amino acid 103 or 181 as well as of clinical isolates resistant to L-697,661 and L-696,229 [3].
  • Enzymes responsible for the hepatic metabolism of L-696,229 in rats were also investigated using various enzyme inducers and polyclonal antibodies to rat P-450 [4].
  • L-696,229 was metabolized by rat liver microsomes to several products: the 5 alpha-hydroxyethyl (M1); 5,6-dihydrodiol (M2); 6'-hydroxy (M3); 6-hydroxymethyl (M4); and 5-vinyl (M5) metabolites [4].
  • The metabolism of L-696,229, 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-o ne, a potent human immunodeficiency virus-type 1 reverse transcriptase inhibitor, by rat liver, lung, gut, and kidney microsomes has been studied [4].

Analytical, diagnostic and therapeutic context of AIDS003337

  • A sensitive high-performance liquid chromatographic (HPLC) method was developed and validated to separate and quantitate the levels of L-696,229 (I), a novel human immunodeficiency virus type I non-nucleoside reverse transcriptase inhibitor, and its hydroxy metabolites (II and III) in plasma samples [5].


  1. Inhibition of HIV-1 reverse transcriptase by pyridinone derivatives. Potency, binding characteristics, and effect of template sequence. Carroll, S.S., Olsen, D.B., Bennett, C.D., Gotlib, L., Graham, D.J., Condra, J.H., Stern, A.M., Shafer, J.A., Kuo, L.C. J. Biol. Chem. (1993) [Pubmed]
  2. L-696,229 specifically inhibits human immunodeficiency virus type 1 reverse transcriptase and possesses antiviral activity in vitro. Goldman, M.E., O'Brien, J.A., Ruffing, T.L., Nunberg, J.H., Schleif, W.A., Quintero, J.C., Siegl, P.K., Hoffman, J.M., Smith, A.M., Emini, E.A. Antimicrob. Agents Chemother. (1992) [Pubmed]
  3. A nonnucleoside reverse transcriptase inhibitor active on human immunodeficiency virus type 1 isolates resistant to related inhibitors. Goldman, M.E., O'Brien, J.A., Ruffing, T.L., Schleif, W.A., Sardana, V.V., Byrnes, V.W., Condra, J.H., Hoffman, J.M., Emini, E.A. Antimicrob. Agents Chemother. (1993) [Pubmed]
  4. In vitro metabolism of L-696,229, an HIV-1 reverse transcriptase inhibitor in rats and humans. Hepatic and extrahepatic metabolism and identification of enzymes involved in the hepatic metabolism. Prueksaritanont, T., Dwyer, L.M., Balani, S.K., Theoharides, A.D. Drug Metab. Dispos. (1994) [Pubmed]
  5. High-performance liquid chromatographic method for the determination of an HIV-1 non-nucleoside reverse transcriptase inhibitor (L-696,229) in plasma samples from animals. Lee, L.L., Herold, M.L., Zacchei, A.G. J. Chromatogr. B, Biomed. Appl. (1996) [Pubmed]
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