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, Tomasz Plech.

Journal Name: Letters in Drug Design & Discovery

Volume 10 , Issue 9 , 2013

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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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Article Details

VOLUME: 10
ISSUE: 9
Year: 2013
Page: [798 - 807]
Pages: 10
DOI: 10.2174/15701808113109990010
Price: $58

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