title: Discovery and evaluation of efficient selenazoles with high antifungal activity against Candida spp.
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 (1)H and (13)C 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.
authors.forename: Krzysztof Z
authors.initials: KZ
authors.lastname: Laczkowski
authors.forename: Konrad
authors.initials: K
authors.lastname: Misiura
authors.forename: Anna
authors.initials: A
authors.lastname: Biernasiuk
authors.affiliation: Department of Chemical Technology and Pharmaceuticals, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Jurasza 2, 85-089 Bydgoszcz, Poland. krzysztof.laczkowski@cm.umk.pl.
authors.forename: Anna
authors.initials: A
authors.lastname: Malm
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002175:Candida / Q000187:drug effects* / Q000254:growth & development; D055808:Drug Discovery; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D016566:Organoselenium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D016566:Organoselenium Compounds