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Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation
Crystallography Unit, School of Physics, Universiti Sains Malaysia, Penang 11800 USM, Malaysia
Department of Chemistry, Alva's Institute of Engineering & Technology, Mijar, Moodbidri 574225, India
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
* Author to whom correspondence should be addressed.
Received: 11 September 2013; in revised form: 1 October 2013 / Accepted: 9 October 2013 / Published: 15 October 2013
Abstract: Chalcone derivatives have attracted increasing attention due to their numerous pharmacological activities. Changes in their structures have displayed high degree of diversity that has proven to result in a broad spectrum of biological activities. The present study highlights the synthesis of some halogen substituted chalcones 3(a–i) containing the 5-chlorothiophene moiety, their X-ray crystal structures and the evaluation of possible biological activities such as antibacterial, antifungal and reducing power abilities. The results indicate the tested compounds show a varied range of inhibition values against all the tested microbial strains. Compound 3c with a p-fluoro substituent on the phenyl ring exhibits elevated antimicrobial activity, whereas the compounds 3e and 3f displayed the least antimicrobial activities. The compounds 3d, 3e, 3f and 3i showed good ferric and cupric reducing abilities, and the compounds 3b and 3c showed the weakest reducing power in the series.
Keywords: heteroaryl; antimicrobial; reducing; substituent; overlay
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Kumar, C.S.C.; Loh, W.-S.; Ooi, C.W.; Quah, C.K.; Fun, H.-K. Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation. Molecules 2013, 18, 12707-12724.
Kumar CSC, Loh W-S, Ooi CW, Quah CK, Fun H-K. Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation. Molecules. 2013; 18(10):12707-12724.
Kumar, C. S.C.; Loh, Wan-Sin; Ooi, Chin W.; Quah, Ching K.; Fun, Hoong-Kun. 2013. "Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation." Molecules 18, no. 10: 12707-12724.