Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation

被引:43
作者
Kumar, C. S. Chidan [1 ,2 ]
Loh, Wan-Sin [1 ]
Ooi, Chin Wei [1 ]
Quah, Ching Kheng [1 ]
Fun, Hoong-Kun [1 ,3 ]
机构
[1] Univ Sains Malaysia, Sch Phys, Xray Crystallog Unit, George Town 11800, Usm, Malaysia
[2] Alvas Inst Engn & Technol, Dept Chem, Mijar 574225, Moodbidri, India
[3] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
关键词
heteroaryl; antimicrobial; reducing; substituent; overlay; ANTIINFLAMMATORY ACTIVITY; ANTIBACTERIAL ACTIVITY; PRENYLATED CHALCONES; CYTOTOXICITY; ANALOGS; DERIVATIVES;
D O I
10.3390/molecules181012707
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
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.
引用
收藏
页码:12707 / 12724
页数:18
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