作者: Shadia A. Galal , Amira S. Abd El-All , Khaled H. Hegab , Asmaa A. Magd-El-Din , Nabil S. Youssef
DOI: 10.1016/J.EJMECH.2010.03.034
关键词: Potency 、 Transition metal 、 Derivative (chemistry) 、 Chemistry 、 Cytotoxicity 、 Benzofuran 、 Medicinal chemistry 、 Ligand 、 Metal 、 Stereochemistry 、 Atevirdine
摘要: Abstract (5-(1 H -benzo[ d ]imidazol-2-yl)-1 -pyrrol-3-yl)(6-hydroxy-4,7-dimethoxybenzofuran-5-yl)methanone (4) and 3-(6-hydroxy-4,7-dimethoxybenzofuran-5-carbonyl)-6 -pyrimido[1,6- a ]pyrimidine-6,8(7 )-dione (5) were synthesized by the reaction of 4,7-dimethoxy-5-oxo-5 -furo[3,2- g ]chromene-6-carbaldehyde (1) with (1 ]imidazol-2-yl)methanamine dihydrochloride and 4-amino-2,6-dihydroxypyrimidine, respectively, via ROR in presence alcoholic KOH. The metal complexes 6-9 compound 4 ; 2 L 1 with (CuCl , FeCl 3 ZnCl LaCl ) 10-13 5 CoCl to form 1:1 or 1:2 (metal: ligand) complexes. HIV inhibitory activity all new compounds was tested. EC 50 values showed that, tested more potent than Atevirdine . Moreover, benzoimidazolylpyrrole derivative (EC = 9 × 10 −6 μM) had higher therapeutic index standard. HIV-1 RT that significant potency but none them HCV NS3-4A protease inhibitor revealed complex formation great positive effect on bioactivity, where Fe-complex 7 most VX-950 Also, cytotoxicity hepatocyte cell line, Cu-complex 10 nearly