从人类免疫缺陷病毒非核苷类逆转录酶抑制剂到强效且选择性的抗锥虫化合物。
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
作者信息
Venkatraj Muthusamy, Ariën Kevin K, Heeres Jan, Joossens Jurgen, Dirié Bertrand, Lyssens Sophie, Michiels Johan, Cos Paul, Lewi Paul J, Vanham Guido, Maes Louis, Van der Veken Pieter, Augustyns Koen
机构信息
Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
Virology Unit, Department of Microbiology, Institute of Tropical Medicine, Nationalestraat 155, B-2000 Antwerp, Belgium.
出版信息
Bioorg Med Chem. 2014 Oct 1;22(19):5241-8. doi: 10.1016/j.bmc.2014.08.005. Epub 2014 Aug 14.
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.
在嘧啶和三嗪非核苷类HIV-1逆转录酶抑制剂文库中存在核苷P2转运体的结构识别基序，促使人们对其抗锥虫活性进行评估。结果表明，抗HIV和抗锥虫活性的构效关系不同。二芳基三嗪系列的优化产生了6-(均三甲氧基)-N2-苯基-1,3,5-三嗪-2,4-二胺(69)，一种具有强大体外抗锥虫活性和中等体内抗锥虫活性的化合物。
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