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Quinolines derivatives as promising new antifungal candidates for the treatment of candidiasis and dermatophytosis
Brazilian Journal of Microbiology ( IF 2.1 ) Pub Date : 2020-07-31 , DOI: 10.1007/s42770-020-00348-4
Gabriella da Rosa Monte Machado 1, 2 , Denise Diedrich 3 , Thaís Carine Ruaro 3 , Aline Rigon Zimmer 3 , Mário Lettieri Teixeira 4 , Luís Flávio de Oliveira 5 , Mickael Jean 6 , Pierre Van de Weghe 6 , Saulo Fernandes de Andrade 1, 3 , Simone Cristina Baggio Gnoatto 3 , Alexandre Meneghello Fuentefria 1, 3
Affiliation  

Fungal infections have emerged as a current serious global public health problem. The main problem involving these infections is the expansion of multidrug resistance. Therefore, the prospection of new compounds with efficacy antifungal becomes necessary. Thus, this study evaluated the antifungal profile and toxicological parameters of quinolines derivatives against Candida spp. and dermatophyte strains. As a result, a selective anti-dermatophytic action was demonstrated by compound 5 (geometric means (GM = 19.14 μg ml−1)). However, compounds 2 (GM = 50 μg ml−1) and 3 (GM = 47.19 μg ml−1) have presented only anti-Candida action. Compounds 3 and 5 did not present cytotoxic action. Compound 5 did not produce dermal and mucosal toxicity. In addition, this compound showed the absence of genotoxic potential, suggesting safety for topical and systemic use. Quinolines demonstrated a potent anti-dermatophytic and anti-yeast action. Moreover, compound 5 presented an excellent toxicological profile, acting as a strong candidate for the development of a new effective and safe compound against dermatophytosis of difficult treatment. Electronic supplementary material The online version of this article (10.1007/s42770-020-00348-4) contains supplementary material, which is available to authorized users.

中文翻译:

喹啉衍生物作为治疗念珠菌病和皮肤癣菌病的新型抗真菌候选药物

真菌感染已成为当前严重的全球公共卫生问题。涉及这些感染的主要问题是多药耐药性的扩大。因此,寻找具有抗真菌功效的新化合物成为必要。因此,本研究评估了喹啉衍生物对念珠菌的抗真菌特性和毒理学参数。和皮肤癣菌菌株。结果,化合物5证明了选择性抗皮肤癣菌作用(几何平均值(GM = 19.14 μg ml-1))。然而,化合物 2 (GM = 50 μg ml-1) 和 3 (GM = 47.19 μg ml-1) 仅具有抗念珠菌作用。化合物3和5没有细胞毒性作用。化合物5不产生皮肤和粘膜毒性。此外,该化合物没有遗传毒性潜力,建议局部和全身使用的安全性。喹啉表现出有效的抗皮肤癣菌和抗酵母菌作用。此外,化合物 5 具有出色的毒理学特征,是开发一种有效且安全的新化合物来对抗难以治疗的皮肤癣菌病的有力候选者。电子补充材料本文的在线版本(10.1007/s42770-020-00348-4)包含补充材料,可供授权用户使用。
更新日期:2020-07-31
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