Scaffold hopping: Exploration of acetanilide-containing uracil analogues as potential NNRTIsстатья
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Дата последнего поиска статьи во внешних источниках: 12 июля 2019 г.
Аннотация:In order to identify novel nonnucleoside inhibitors of HIV-1 reverse transcriptase two series of amide-containing uracil derivatives were designed as hybrids of two scaffolds of previously reported inhibitors. Subsequent biological evaluation confirmed acetamide uracil derivatives 15a-k as selective micromolar NNRTIs with a first generation-like resistance profile. Molecular modeling of the most active compounds 15c and 15i was employed to provide insight on their inhibitory properties and direct future design efforts. (C) 2015 Elsevier Ltd. All rights reserved.