Discovery and Evaluation of Efficient Selenazoles with High Antifungal Activity Against Candida spp.

Title:Discovery and Evaluation of Efficient Selenazoles with High Antifungal Activity Against Candida spp.

Volume: 11 Issue: 2

Author(s): Krzysztof Z. Laczkowski, Konrad Misiura, Anna Biernasiuk and Anna Malm

Affiliation:

Keywords: Selenazoles, selenosemicarbazones, antimicrobial drugs, gram-positive bacteria, gram-negative bacteria, DFT calculation.

Abstract: Synthesis, characterization and investigation of antifungal and antibacterial activities of fourteen 2,4- disubstituted 1,3-selenazoles is presented. Their structures were determined using ¹H and ¹³C NMR, FAB MS and HRMS analyses. Among the derivatives, compounds 5, 6, 8, 9, 12, 13 and 15 had very strong activity against reference strains of C. albicans ATCC 10231 and C. parapsilosis ATCC 22019 with MIC = 0.24-7.81 µg/ml. The compounds 5, 6, 8, 13 and 15 showed also very strong activity against clinical isolates belonging to non-albicans Candida spp. strains, i.e. C. krusei, C. inconspicua, C. famata, C. lusitaniae, C. sake, C. parapsilosis, C. dubliniensis with MIC = 0.24-7.81 µg/ml. The activity of several of these was similar to the activity of most commonly used antifungal agents fluconazole. The compounds 9 and 16 indicate also very strong antibacterial activity against S. epidermidis and M. luteus with MIC = 1.95-3.91 µg/ml. Additionally, the compound 11 is strong active against M. luteus with MIC = 3.91 µg/ml.

Cite this article as:

Laczkowski Z. Krzysztof, Misiura Konrad, Biernasiuk Anna and Malm Anna, Discovery and Evaluation of Efficient Selenazoles with High Antifungal Activity Against Candida spp., Medicinal Chemistry 2015; 11 (2) . https://dx.doi.org/10.2174/1573406410666140826111121