Burmaoglu Serdar, Algul Oztekin, Gobek Arzu, Aktas Anil Derya, Ulger Mahmut, Erturk Busra Gul, Kaplan Engin, Dogen Aylin, Aslan Gönül
a Tercan Vocational High School, Erzincan University , Erzincan , Turkey.
b Department of Chemistry, Faculty of Science , Ataturk University , Erzurum , Turkey.
J Enzyme Inhib Med Chem. 2017 Dec;32(1):490-495. doi: 10.1080/14756366.2016.1265517.
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 IC 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.
由于细菌和真菌的耐药性不断增加，我们试图开发新型抗结核和抗菌药物。为此，我们采用构效关系方法开发了一些新的氟取代查尔酮类似物（3、4、9 - 15以及20 - 23）。对目标化合物进行了抗结核分枝杆菌H37Rv的抗结核疗效评估以及对五种常见致病细菌和三种常见真菌菌株的抗菌活性评估。三种衍生物（3、9和10）表现出显著的抗结核活性，IC值≤16,760。与相应的羟基类似物相比，查尔酮结构B环上具有单氟取代的三甲氧基取代基支架衍生的化合物表现出更强的抑制活性。在抗菌活性方面，大多数化合物（3、9、12 - 14和23）对细菌表现出中度至强效活性，化合物3、13、15、20和22的抗真菌活性与参考药物氨苄青霉素和氟康唑相当。
