Synthesis, in Vitro Biological Screening and Molecular Docking Studies of Novel Camphor Based Thiazoles

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Editor-in-Chief:
Atta-ur-Rahman, FRS
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Kings College
University of Cambridge
Cambridge
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Synthesis, in Vitro Biological Screening and Molecular Docking Studies of Novel Camphor Based Thiazoles

Author(s): Krzysztof Z. Łączkowski, Konrad Misiura, Anna Biernasiuk, Anna Malm, Agata Siwek, Tomasz Plech, Emilia Ciok-Pater, Krzysztof Skowron and Eugenia Gospodarek

Affiliation: Department of Chemical Technology and Pharmaceuticals, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Jurasza 2, 85-089 Bydgoszcz, Poland

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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Article Details

Volume: 10
First Page: 1
Page Count: 1
DOI: 10.2174/1573406410666140714130743
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