1-(2,6-二氟苯基)-1H,3H-噻唑并[3,4-a]苯并咪唑结构相关的1,2-取代苯并咪唑的合成及抗HIV活性
Synthesis and anti-hIV activity of 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole structurally-related 1,2-substituted benzimidazoles.
作者信息
Rao Angela, Chimirri Alba, De Clercq Erik, Monforte Anna Maria, Monforte Pietro, Pannecouque Christophe, Zappalà Maria
机构信息
Dipartimento Farmaco-Chimico, Università di Messina, Italy.
出版信息
Farmaco. 2002 Oct;57(10):819-23. doi: 10.1016/s0014-827x(02)01300-9.
The synthesis of 1,2-substituted benzimidazoles is reported. These novel derivatives share chemical similarities with 1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles, a class of HIV-1 NNRTIs studied widely. All compounds prepared were tested in MT-4 cells to explore their potential anti-HIV activity and were found to be less potent than 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole (TBZ).
报道了1,2-取代苯并咪唑的合成。这些新型衍生物与1-芳基-1H,3H-噻唑并[3,4-a]苯并咪唑具有化学相似性，后者是一类已被广泛研究的HIV-1非核苷类逆转录酶抑制剂。所制备的所有化合物均在MT-4细胞中进行了测试，以探索其潜在的抗HIV活性，结果发现它们的活性均低于1-(2,6-二氟苯基)-1H,3H-噻唑并[3,4-a]苯并咪唑（TBZ）。
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