El Azab Islam H, Youssef Mohamed M, Amin Mahmoud A
Chemistry Department, Faculty of Science, Taif University, Al-Haweiah, P.O. Box 888, Taif 21974, Saudi Arabia.
Chemistry Department, Faculty of Science, Aswan University, Aswan 81528, Egypt.
Molecules. 2014 Nov 26;19(12):19648-64. doi: 10.3390/molecules191219648.
6-Hydroxy-2-oxo-2H-chromene-4-carbaldehyde (2), 6-chloro-2-oxo-2H-chromene-4-carbaldehyde (3) and 6-hydrazinyl-4-methyl-2H-chromen-2-one (5) were prepared as single-pharmacophore motif key intermediates. Compounds 2, 3 and 5 were incorporated in a series of multicomponent reactions (MCRs), under microwave assistance as well as conventional chemical synthesis processes, to afford a series of three and/or four-pharmacophoric-motif conjugates 8a,b, 11, 13, 16, 17, 19 and 20 in good yields. The newly synthesized compounds were characterized by IR, NMR, 13C-NMR, MS and elemental analyses. Finally the synthesized compounds have been screened for their biological activity whereupon they exhibited remarkable antimicrobial activity on different classes of bacteria and the fungus.
制备了6-羟基-2-氧代-2H-色烯-4-甲醛（2）、6-氯-2-氧代-2H-色烯-4-甲醛（3）和6-肼基-4-甲基-2H-色烯-2-酮（5）作为单药效基团基序关键中间体。在微波辅助以及传统化学合成过程中，将化合物2、3和5引入一系列多组分反应（MCR）中，以良好的产率得到一系列三药效基团和/或四药效基团共轭物8a、b、11、13、16、17、19和20。通过红外光谱（IR）、核磁共振（NMR）、13C-核磁共振（13C-NMR）、质谱（MS）和元素分析对新合成的化合物进行了表征。最后，对合成的化合物进行了生物活性筛选，结果显示它们对不同种类的细菌和真菌表现出显著的抗菌活性。
