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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3- Thiazoles

Author(s): Krzysztof Z.  Laczkowski, Konrad Misiura, Anna Biernasiuk, Anna Malm, Agata Siwek and Tomasz Plech

Volume 10, Issue 9, 2013

Page: [798 - 807] Pages: 10

DOI: 10.2174/15701808113109990010

Price: $65

Abstract

Synthesis, characterization and investigation of antibacterial and antifungal activities of thirteen novel 6- hydroxybenzofuran-3(2H)-one based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using NMR, FAB MS and HRMS analyses. The results of microbiological screening reveal that three derivatives containing fluorine, bromine and hydrogen substituents at the phenyl ring are the most active antimicrobial compounds. Molecular docking studies of all compounds on the active sites of microbial enzymes indicated a possible target Nmyristoyltransferase (NMT).

Keywords: Thiazoles, Thiosemicarbazones, Benzofuranone, Antimicrobial drugs, N-myristoyltransferase, Molecular modeling.


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