Design of potent fluoro-1substituted chalcones as antimicrobial agents

作者：Burmaoglu Serdar; Algul Oztekin; Gobek Arzu; Anil Derya Aktas; Ulger Mahmut; Erturk Busra Gul; Kaplan Engin; Dogen Aylin; Aslan Gonul

来源：Journal of Enzyme Inhibition and Medicinal Chemistry, 2017, 32(1): 490-495.

DOI：10.1080/14756366.2016.1265517

• Chalcone
• antitubercular activity
• antimicrobial activity
• SAR

Owing to ever-increasing bacterial and fungal drug resistance, we attempted to develop novel antitubercular and antimicrobial agents. For this purpose, we developed some new fluorine-substituted chalcone analogs (3, 4, 9-15, and 20-23) using a structure-activity relationship approach. Target compounds were evaluated for their antitubercular efficacy against Mycobacterium tuberculosis H37Rv and antimicrobial activity against five common pathogenic bacterial and three common fungal strains. Three derivatives (3, 9, and 10) displayed significant antitubercular activity with IC50 values of <= 16,760. Compounds derived from trimethoxy substituent scaffolds with monofluoro substitution on the B ring of the chalcone structure exhibited superior inhibition activity compared to corresponding hydroxy analogs. In terms of antimicrobial activity, most compounds (3, 9, 12-14, and 23) exhibited moderate to potent activity against the bacteria, and the antifungal activities of compounds 3, 13, 15, 20, and 22 were comparable to those of reference drugs ampicillin and fluconazole.

• 出版日期2017