新型咪唑并[2,1-b]-1,3,4-噻二唑作为抗新型隐球菌临床分离株的有前景的抗真菌剂。
Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans.
作者信息
Alwan Wesam S, Karpoormath Rajshekhar, Palkar Mahesh B, Patel Harun M, Rane Rajesh A, Shaikh Mahamadhanif S, Kajee Afsana, Mlisana Koleka P
机构信息
Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
出版信息
Eur J Med Chem. 2015 May 5;95:514-25. doi: 10.1016/j.ejmech.2015.03.021. Epub 2015 Mar 12.
We herein report the synthesis and in vitro antimicrobial evaluation of twenty five novel hybrid derivatives of imidazo [2,1-b]-1,3,4-thiadiazole containing chalcones (5a-o) and Schiff bases (6a-j) against three fungal strains (Candida albicans, Cryptococcus neoformans and Aspergillus niger). Most of the tested compounds displayed substantial anti-fungal activity with MICs ranging between 1.56 and 100 μg/mL. Compounds 5a, 5b and 5n exhibited promising activity against C. neoformans at a MIC 1.56 μg/mL. In addition, compound 5n also demonstrated significant antifungal activity against the clinical isolates of C. neoformans at MIC 3.125 μg/mL. However, moderate activity was observed for these compounds against four bacterial strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and Mycobacterium tuberculosis (H37Rv).
我们在此报告了含查尔酮（5a - o）和席夫碱（6a - j）的25种新型咪唑并[2,1 - b]-1,3,4 - 噻二唑杂化衍生物对三种真菌菌株（白色念珠菌、新型隐球菌和黑曲霉）的合成及体外抗菌评估。大多数测试化合物表现出显著的抗真菌活性，最低抑菌浓度（MIC）范围在1.56至100μg/mL之间。化合物5a、5b和5n对新型隐球菌表现出有前景的活性，MIC为1.56μg/mL。此外，化合物5n对新型隐球菌临床分离株在MIC为3.125μg/mL时也表现出显著的抗真菌活性。然而，观察到这些化合物对四种细菌菌株（金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌和铜绿假单胞菌）以及结核分枝杆菌（H37Rv）具有中等活性。
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