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.
Letters in Drug Design & Discovery
Title:Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3- Thiazoles
Volume: 10 Issue: 9
Author(s): Krzysztof Z. Laczkowski, Konrad Misiura, Anna Biernasiuk, Anna Malm, Agata Siwek and Tomasz Plech
Affiliation:
Keywords: Thiazoles, Thiosemicarbazones, Benzofuranone, Antimicrobial drugs, N-myristoyltransferase, Molecular modeling.
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).
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Laczkowski Z. Krzysztof, Misiura Konrad, Biernasiuk Anna, Malm Anna, Siwek Agata and Plech Tomasz, Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3- Thiazoles, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/15701808113109990010
DOI https://dx.doi.org/10.2174/15701808113109990010 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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