[Pharmacological importance of novel spiro derivatives against human pathogenic fungi].

Q3 Biochemistry, Genetics and Molecular Biology
G Sharma, R Sharma, R Saxena, E Rajni, V Prakash Mamoria
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引用次数: 0

Abstract

Human mycoses have become a threat to health world-wide. Unfortunately there are only a limited number of antimycotic drugs in use. In the present study, antifungal activity of earlier synthesized spiro-1,4-dihydropyridines (1,4-DHPs) was investigated. The antifungal activity of spiro-1,4-DHPs compounds were screened against Aspergillus flavus, A. fumigatus, and Candida albicans by using Disc Diffusion and Modified Microdilution method. Among six spiro-1,4-DHPs compounds tested all of them showed stronger antifungal activity possibly through inhibiting the synthesis of chitin in cell wall against A. flavus, A. fumigatus, and C. albicans as compared to fluconazole, a standard antifungal drug. The combination of compounds showed that the synthesized compounds had synergistic, additive effects as compared to currently used drugs as an antifungal agent. These results indicated that these designed compounds were potential chitin synthase inhibitors and had excellent antimycotic activity for the treatment of fungal infections.

[新型螺旋衍生物对人类致病真菌的药理意义]。
人类真菌病已成为对全世界健康的威胁。不幸的是,目前使用的抗真菌药物数量有限。本研究对早期合成的螺-1,4-二氢吡啶(1,4- dhps)的抗真菌活性进行了研究。采用圆盘扩散法和改良微量稀释法对spiro-1,4- dhps化合物对黄曲霉、烟曲霉和白色念珠菌的抑菌活性进行了筛选。在所检测的6种spio -1,4- dhps化合物中,与标准抗真菌药物氟康唑相比,它们对黄曲霉、烟曲霉和白色念珠菌均表现出更强的抗真菌活性,可能是通过抑制细胞壁几丁质的合成。化合物的组合表明,与目前使用的抗真菌药物相比,合成的化合物具有增效、加性作用。这些结果表明,所设计的化合物是潜在的几丁质合成酶抑制剂,对真菌感染具有良好的抗真菌活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Biomeditsinskaya khimiya
Biomeditsinskaya khimiya Biochemistry, Genetics and Molecular Biology-Biochemistry, Genetics and Molecular Biology (all)
CiteScore
1.30
自引率
0.00%
发文量
49
期刊介绍: The aim of the Russian-language journal "Biomeditsinskaya Khimiya" (Biomedical Chemistry) is to introduce the latest results obtained by scientists from Russia and other Republics of the Former Soviet Union. The Journal will cover all major areas of Biomedical chemistry, including neurochemistry, clinical chemistry, molecular biology of pathological processes, gene therapy, development of new drugs and their biochemical pharmacology, introduction and advertisement of new (biochemical) methods into experimental and clinical medicine etc. The Journal also publish review articles. All issues of journal usually contain invited reviews. Papers written in Russian contain abstract (in English).
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