The inhibitory activity of diazinyl-substituted thiourea derivatives on human immunodeficiency virus type 1 reverse transcriptase

被引:22
作者
Heinisch, G [1 ]
Matuszczak, B [1 ]
Pachler, S [1 ]
Rakowitz, D [1 ]
机构
[1] UNIV INNSBRUCK, INST PHARMACEUT CHEM, A-6020 INNSBRUCK, AUSTRIA
关键词
non-nucleoside HIV reverse transcriptase inhibitor; pyridazine; pyrimidine; pyrazine; diazinyl-substituted thioureas;
D O I
10.1177/095632029700800507
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Starting from 2-(2-aminoethyl)pyridine, a series of N-daizinyl-N'-[2-(2-pyridyl)ethyl]thioureas was prepared via the (2-pyridyl)ethylisothiocyanate and was screened as non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. Derivatives bearing a 3-pyridazinyl or a 4-pyrimidinyl moiety turned out to be the most potent compounds. However, they exhibited less activity than nevirapine or trovirdine.
引用
收藏
页码:443 / 446
页数:4
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