Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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

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

Graphical Abstract:


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.

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

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Article Details

VOLUME: 11
ISSUE: 2
Year: 2015
Page: [118 - 127]
Pages: 10
DOI: 10.2174/1573406410666140826111121
Price: $58