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N'-[2-(2-thiophene) ethyl]-N'-[2-(5-bromopyridyl)]thiourea (HI-443), a rationally designed non-nucleoside reverse transcriptase inhibitor compound with potent anti-HIV activity.

作者信息

Uckun Fatih M, Qazi Sanjive, Venkatachalam Taracad

机构信息

Paradigm Pharmaceuticals, 2139 Fourth Street, White Bear Lake, MN 55110, USA.

出版信息

Arzneimittelforschung. 2007;57(5):278-85. doi: 10.1055/s-0031-1296619.

DOI:10.1055/s-0031-1296619
PMID:17598700
Abstract

The in vitro activity profile of N'- [2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea (CAS 258340-15-7, HI-443) was examined against 38 clinical isolates of HIV-1. HI-443 inhibited the replication and/or infectivity of each of the 7 HIV-1 isolates of non-B envelope subtype, each of the 22 isolates with genotypic nucleoside reverse transcriptase inhibitor (NRTI) resistance, each of the 6 multidrug-resistant HIV isolates with genotypic NRTI/non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance, each of the 3 isolates with no RT mutations, and each of the 3 laboratory strains of HIV-I with NNRTI or NNRTI/NRTI resistance. The potency of HI-443 against clinical HIV-1 isolates with NRTI- or NNRTI-resistance warrants the further development of this rationally designed NNRTI as a new anti-HIV agent.

摘要

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