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).