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  • Title: Synthesis, in vitro biological screening and molecular docking studies of novel camphor-based thiazoles.
    Author: Laczkowski KZ, Misiura K, Biernasiuk A, Malm A, Siwek A, Plech T, Ciok-Pater E, Skowron K, Gospodarek E.
    Journal: Med Chem; 2014; 10(6):600-8. PubMed ID: 25019315.
    Abstract:
    Synthesis, 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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