Synthesis of β-fluorophenethyl halopyridyl thiourea compounds as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Synthesis of β-fluorophenethyl halopyridyl thiourea compounds as non-nucleoside inhibitors of HIV-1 reverse transcriptase
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DOI：
10.1081/scc-120039500
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发表时间：
2004-06-01
影响因子：
2.1
通讯作者：
Uckun, FM
中科院分区：
文献类型：
--
作者：
Venkatachalam, TK;Uckun, FM
以三步反应合成了β-氟苯乙胺类化合物，总收率为50%。β-氟苯乙胺盐酸盐与由卤代吡啶胺衍生的硫代羰基咪唑衍生物在二甲基甲酰胺中缩合，得到所需的硫脲化合物，为结晶固体。几种β-氟苯乙基硫脲化合物在纳摩尔至低微摩尔浓度下抑制HIV-1逆转录酶（RT）。
Synthesis of beta-fluorophenethylamines was accomplished in three steps with an overall yield of 50%. Condensation of beta-fluorophenethylamine hydrochloride with thiocarbonylimidazole derivative derived from halopyridyl amines in dimethylformamide furnished the desired thiourea compounds as crystalline solids. Several of the beta-fluorophenethyl thiourea compounds inhibited HIV-1 reverse transcriptase (RT) at nanomolar to low micromolar concentrations.