新型螺[吲哚啉-3,2'噻唑并[5,4-e]嘧啶并[1,2-a]嘧啶]衍生物作为可能的抗皮肤癣菌和抗念珠菌药。

Q3 Biochemistry, Genetics and Molecular Biology
G Sharma, R Sharma
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引用次数: 0

摘要

合成了一系列新型 5'-benzylidene-3'-phenylspiro[indoline-3,2'-thiazolidine]-2,4'(1H)-diones 6a-d 和 spiro[indoline-3,2'-thiazolo[5,4-e]pyrimido[1,2-a]pyrimidin]-2(1H)-one 9a-d 衍生物。采用圆盘扩散法和改良微量稀释法评估了所有新合成化合物的抗真菌和抗念珠菌活性。抗菌实验表明,合成的化合物在体外具有广谱抗真菌活性。其中,化合物 9a-9d 对红色毛癣菌、白色毛癣菌和白色念珠菌具有较强的抗真菌活性;与抗真菌参考药物酮康唑相比,化合物 6a-d 对某些真菌菌株也具有显著的抗真菌活性。对抗药性真菌变种的抗真菌活性评估表明,设计的化合物对测试的变种具有显著的抗真菌活性。化合物(6a-d)和(9a-d)的组合显示合成的化合物具有协同效应或相加效应。这些结果表明,合成的化合物是假定的几丁质合成酶抑制剂,具有广谱抗真菌活性。本研究结果表明,新型螺嘧啶衍生物可用作治疗皮肤癣菌病和其他真菌病的新型候选药物的活性药物成分。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel spiro[indoline-3,2'thiazolo[5,4-e]pyrimido[1,2-a] pyrimidine] derivatives as possible anti-dermatophytic and anti-candidiasis agent.

A novel series of 5'-benzylidene-3'-phenylspiro[indoline-3,2'-thiazolidine]-2,4'(1H)-diones 6a-d and spiro[indoline-3,2'-thiazolo[5,4-e]pyrimido[1,2-a]pyrimidin]-2(1H)-one 9a-d derivatives have been synthesized. All the newly synthesized compounds were evaluated for antifungal and anti-candidiasis activity by using Disc Diffusion and Modified Microdilution methods. The antimicrobial experiments have shown that the synthesized compounds demonstrated broad-spectrum antifungal activity in vitro. Among them, compounds 9a-9d had stronger antifungal activity against Trichophyton rubrum, Trichophyton mentagrophytes, and Candida albicans; compounds 6a-d also showed significant antifungal activity against selected fungal strains as compared to ketoconazole, the reference antifungal drug. The evaluation of antifungal activity against drug-resistant fungal variants showed that the designed compounds had significant antifungal activity against the tested variants. The combination of compounds (6a-d) and (9a-d) exhibited that the synthesized compounds had synergistic effects or additive effects. These results demonstrated that the synthesized compounds were putative chitin synthase inhibitors exhibiting broad spectrum antifungal activities. The present results indicate that novel spiro pyrimidine derivatives can be used as an active pharmaceutical ingredient for novel drug candidate for treatment of dermatophytosis and other fungal agents.

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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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