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From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. 2014
Muthusamy Venkatraj, and
Kevin K Ariën, and
Jan Heeres, and
Jurgen Joossens, and
Bertrand Dirié, and
Sophie Lyssens, and
Johan Michiels, and
Paul Cos, and
Paul J Lewi, and
Guido Vanham, and
Louis Maes, and
Pieter Van der Veken, and
Koen Augustyns
Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
The presence of a structural recognition motif for the nucleoside P2 transporter in a library of pyrimidine and triazine non-nucleoside HIV-1 reverse transcriptase inhibitors, prompted for the evaluation of antitrypanosomal activity. It was demonstrated that the structure-activity relationship for anti-HIV and antitrypanosomal activity was different. Optimization in the diaryl triazine series led to 6-(mesityloxy)-N2-phenyl-1,3,5-triazine-2,4-diamine (69), a compound with potent in vitro and moderate in vivo antitrypanosomal activity.
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