具有抗真菌活性的螺旋菌吲哚-吡咯烷杂环杂交种的发现。

IF 2.7 4区医学 Q3 IMMUNOLOGY

Pathogens and disease Pub Date : 2022-05-05 DOI:10.1093/femspd/ftac013

H. Dowdy, Raju Suresh Kumar, A. Almansour, N. Arumugam, Shatha IbrahimAlaqeel, Shankar Thangamani

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引用次数: 0

摘要

真菌病原体主要是念珠菌和隐球菌，对人类造成严重的危及生命的感染，特别是在免疫功能低下的个体中。越来越多的抗真菌药物耐药性以及fda批准的药物的缺乏表明迫切需要新的抗真菌药物。我们对新合成的螺氧吲哚杂环杂化化合物的筛选表明，新的小分子DPA-3具有有效的抗真菌活性，而不会诱导哺乳动物细胞毒性。此外，DPA-3显著减少白色念珠菌ATCC 10231菌株的菌丝和生物膜形成，优于FDA批准的两种抗真菌药物。我们的研究结果表明，DPA-3作为一种抗真菌药物具有进一步开发的潜力。

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Discovery of spirooxindole-pyrrolidine heterocyclic hybrids with potent antifungal activity against fungal pathogens.

Fungal pathogens mainly Candida and Cryptococcus species causes serious life-threating infections to humans, especially in individuals who are immunocompromised. Increasing frequency of antifungal drug resistance along with paucity of FDA-approved drugs suggest a dire need for new antifungal drugs. Our screening of newly synthesized spirooxindole heterocyclic hybrid compounds revealed that the novel small molecule, DPA-3, has potent antifungal activity without inducing mammalian cell cytotoxicity. Furthermore, DPA-3 significantly reduced hyphal and biofilm formation of Candida albicans ATCC 10231 strain, out-competing two FDA approved antifungal drugs. The results of our study conclude that DPA-3 is a compelling candidate for further development as an antifungal drug.

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来源期刊

Pathogens and disease IMMUNOLOGY-INFECTIOUS DISEASES

CiteScore

7.40

自引率

3.00%

发文量

期刊介绍： Pathogens and Disease publishes outstanding primary research on hypothesis- and discovery-driven studies on pathogens, host-pathogen interactions, host response to infection and their molecular and cellular correlates. It covers all pathogens – eukaryotes, prokaryotes, and viruses – and includes zoonotic pathogens and experimental translational applications.