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Arzneimittelforschung 2007; 57(6): 330-338
DOI: 10.1055/s-0031-1296627
Antibiotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Large-scale Synthesis of GMP Grade N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443), a New Anti-HIV Drug Candidate

Darin DuMez
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Taracad K. Venkatachalam
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Fatih M. Uckun
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
› Author Affiliations
Further Information

Publication History

Publication Date:
21 December 2011 (online)

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Abstract

The thiourea compound N'-[2-(2-thio-phene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443, CAS 258340-15-7), was found to be a potent anti-HIV agent with remarkable activity against nucleoside analog reverse transcriptase (NRT)-resis-tant, non-nucleoside analog reverse transcriptase (NNRT) -resistant, as well as multidrug-resistant HIV. Now the method of producing HI-443 under current Good Manufacturing Practice (cGMP) conditions on the scale of kilograms is reported. The availability of GMP-grade HI-443 will promote the preclinical and clinical development efforts aimed at making this new drug candidate available to HIV-infected persons.

Key words

Anti-HIV agents - CAS 258340-15-7 - HI-443 - N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea - Non-nucleoside analog reverse transcriptase inhibitors