Microwave-Assisted Synthesis of Novel 2H-Chromene Derivatives Bearing Phenylthiazolidinones and Their Biological Activity Assessment

Molecules

Islam H. El Azab¹  Mohamed M. Youssef³  Mahmoud A. Amin² 

[1] Chemistry Department, Faculty of Science, Aswan University, Aswan 81528, Egypt;Chemistry Department, Faculty of Science, Taif University, Al-Haweiah, P.O. Box 888, Taif 21974, Saudi Arabia;Chemistry Department, Faculty of Science, Cairo University, Giza 12613, Egypt

关键词: multicomponent reactions (MCRs);    green synthesis;    microwave irradiation;    2-H-chromene;    thiazolidenone;    biological activity;   

DOI  :  10.3390/molecules191219648

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.