Chemistry and Chemical Processing Technology, Kocaeli Vocational School, Kocaeli University, Kocaeli, Turkey.
Department of Microbiology, Faculty of Medicine, Kocaeli University, Kocaeli, Turkey.
Braz J Microbiol. 2022 Sep;53(3):1297-1303. doi: 10.1007/s42770-022-00777-3. Epub 2022 Jun 13.
The aim of this study was to investigate the in vitro activity of thirty-eight heterocyclic organoboron compounds (1a-o, 2a-j, 3a-m) against clinically isolated dermatophytes Trichophyton mentagrophytes and Microsporum canis. Minimum inhibitory concentrations (MICs) of compounds (1a-o, 2a-j, 3a-m) were determined according to published protocol Clinical and Laboratory Standards Institute (CLSI) M38-A2 broth microdilution method. The minimum fungicidal concentrations (MFCs) for both T. mentagrophytes and M. canis were found by subculturing each fungal suspension on potato dextrose agar. According to the results, heterocyclic organoboron compounds (1a-o, 2a-j, 3a-m) were found to be more effective against dermatophyte M. canis (MIC = 3.12-25 µg/ml) than T. mentagrophytes (MIC = 12.5-100 µg/ml). Our findings showed that 7-membered heterocyclic organoboron compounds (3a-m) (MIC = 12.5-50 µg/ml) have stronger in vitro antifungal activity against T. mentagrophytes than 5-membered heterocyclic organoboron compounds (1a-o, 2a-j) (MIC = 25-100 µg/ml). The MFC values for all compounds ranged from 6.25 to 200 µg/ml. The limited number of systemic antifungal agents used in the treatment of dermatophyte infections and the presence of side effects have led to the search for new treatment resources in recent years. Therefore, investigation of the effect of heterocyclic organoboron compounds against dermatophytes will be promising for the discovery of new antifungal compounds that have gained great importance today.
本研究旨在研究 38 种杂环有机硼化合物（1a-o、2a-j、3a-m）对临床分离的皮肤癣菌须癣毛癣菌和犬小孢子菌的体外活性。根据已发表的方案临床和实验室标准协会（CLSI）M38-A2 肉汤微量稀释法测定化合物（1a-o、2a-j、3a-m）的最小抑菌浓度（MIC）。通过将真菌混悬液在土豆葡萄糖琼脂上连续传代，确定须癣毛癣菌和犬小孢子菌的最低杀菌浓度（MFC）。结果表明，杂环有机硼化合物（1a-o、2a-j、3a-m）对皮肤癣菌犬小孢子菌（MIC=3.12-25μg/ml）的作用比须癣毛癣菌（MIC=12.5-100μg/ml）更有效。我们的研究结果表明，7 元杂环有机硼化合物（3a-m）（MIC=12.5-50μg/ml）对须癣毛癣菌的体外抗真菌活性强于 5 元杂环有机硼化合物（1a-o、2a-j）（MIC=25-100μg/ml）。所有化合物的 MFC 值范围为 6.25-200μg/ml。近年来，由于用于治疗皮肤癣菌感染的全身性抗真菌药物数量有限且存在副作用，因此一直在寻找新的治疗资源。因此，研究杂环有机硼化合物对皮肤癣菌的作用对于发现新的抗真菌化合物具有重要意义。
