新型非核苷类HIV-1逆转录酶抑制剂1-[(烯基或炔基或烷氧基)甲基]-5-烷基-6-(1-萘甲酰基)-2,4-嘧啶二酮的合成及抗HIV活性评价
Synthesis and anti-HIV activity evaluation of 1-[(alkenyl or alkynyl or alkyloxy)methyl]-5-alkyl-6-(1-naphthoyl)-2,4-pyrimidinediones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
作者信息
Ji Lei, Chen Fen-Er, Xie Bin, De Clercq Erik, Balzarini Jan, Pannecouque Christophe
机构信息
Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
出版信息
Eur J Med Chem. 2007 Feb;42(2):198-204. doi: 10.1016/j.ejmech.2006.09.018. Epub 2006 Nov 13.
The synthesis and anti-HIV activity evaluation of a new series of 2,4-pyrimidinediones bearing a 6-(1-naphthoyl) group are described. In general, it was found that most of the title compounds showed good activities against human immunodeficiency virus type-1 (HIV-1). In particular, compound 26 displayed the most potent anti-HIV-1 activity (IC(50)=0.11+/-0.05 microM), inhibiting HIV-1 replication in MT-4 cells more effectively than HEPT (by 45-fold) and DDI (by 50-fold).
描述了一系列带有6-(1-萘甲酰基)基团的新型2,4-嘧啶二酮的合成及其抗HIV活性评估。总体而言，发现大多数标题化合物对1型人类免疫缺陷病毒(HIV-1)表现出良好的活性。特别是，化合物26表现出最有效的抗HIV-1活性(IC(50)=0.11±0.05 microM)，在MT-4细胞中抑制HIV-1复制的效果比HEPT(高45倍)和DDI(高50倍)更有效。
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