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Bioorg Med Chem Lett. 2011 Jul 1;21(13):3935-8. doi: 10.1016/j.bmcl.2011.05.020. Epub 2011 May 14.

Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.

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European Research Centre for Drug Discovery and Development (NatSynDrugs), via Aldo Moro, 2-Università di Siena, 53100 Siena, Italy.


We investigated some pyrrolobenzoxazepinone (PBOs, 3e-i) analogues of early described effective non-nucleoside inhibitors of HIV-1 reverse transcriptase (RT). Enzymological studies of 3e-i enantiomers, with wild type (wt) RT and some drug-resistant mutants, revealed a stereoselective mode of action and selectivity for RT ternary complex. Unexpectedly (+)-3g was found more potent towards the L100I mutant than towards the wt RT, whereas (+)-3h inhibited the K103N mutant and RT wt with comparable potency.

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