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Arzneimittelforschung 2007; 57(5): 278-285
DOI: 10.1055/s-0031-1296619
Antibiotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

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

Fatih M. Uckun
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Sanjive Qazi
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Taracad Venkatachalam
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
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Publikationsverlauf

Publikationsdatum:
21. Dezember 2011 (online)

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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 multi-drug-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-1 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 agents.

Key words

Anti-HIV agents - CAS 258340-15-7 - HI-443, in vitro anti-HIV activity profile - Non-nucleoside reverse - transcriptase inhibitors - N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea