Synthesis, in Vitro Biological Screening and Molecular Docking Studies of Novel Camphor Based Thiazoles
Krzysztof Z. Łączkowski, Konrad Misiura, Anna Biernasiuk, Anna Malm, Agata Siwek, Tomasz Plech, Emilia Ciok-Pater, Krzysztof Skowron and Eugenia GospodarekAffiliation:
Department of Chemical Technology and Pharmaceuticals, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Jurasza 2, 85-089 Bydgoszcz, Poland
AbstractSynthesis, characterization and investigation of antibacterial and antifungal activities of twelve camphor based 2,4-disubstituted 1,3-thiazoles is presented. Their structures were determined using NMR, IR, FAB MS and HRMS analyses. Among the derivatives, 3i and 5 were found to exhibit antifungal and antibacterial activities comparable to that of fluconazole and ciprofloxacin against yeast belonging to Candida spp., MIC 0.12-0.98 µg/ml and Gram-positive bacteria including both pathogenic S. aureus and opportunistic S. epidermidis, MIC 0.98-7.81 µg/ml, B. subtilis and B. cereus, MIC 3.91-31.25 µg/ml, and M. luteus, MIC 0.98 µg/ml species, respectively. Molecular docking studies of all compounds into the active sites of microbial enzymes indicated a possible targets SAP and NMT, thiazoles 3a-j, 4, 5 showed more favourable affinity than the native ligand.
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