Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans

作者：Alwan Wesam S; Karpoormath Rajshekhar^*; Palkar Mahesh B; Patel Harun M; Rane Rajesh A; Shaikh Mahamadhanif S; Kajee Afsana; Mlisana Koleka P

来源：European Journal of Medicinal Chemistry, 2015, 95: 514-525.

DOI：10.1016/j.ejmech.2015.03.021

• Imdazo [2,1-b]-1,3,4-thiadiazole
• Chalcones
• Schiff bases
• Antifungal activity
• Cryptococcosis
• Ciyptococcus neoformans

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 Asperg-illus niger). Most of the tested compounds displayed substantial anti-fungal activity with MICs ranging between 1.56 and 100 mu g/mL. Compounds 5a, 5b and 5n exhibited promising activity against C neoformans at a MIC 1.56 mu g/mL. In addition, compound 5n also demonstrated significant antifungal activity against the clinical isolates of C neoformans at MIC 3.125 mu g/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 (H(37)Rv).

• 出版日期2015-5-5