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

被引：0

作者：

Laczkowski, Krzysztof Z. ^{[1
]}

Misiura, Konrad ^{[1
]}

Biernasiuk, Anna ^{[2
]}

Malm, Anna ^{[2
]}

Siwek, Agata ^{[3
]}

Plech, Tomasz ^{[3
]}

机构：

[1] Nicholas Copernicus Univ, Fac Pharm, Dept Chem Technol & Pharmaceut, Coll Med, PL-85089 Bydgoszcz, Poland

[2] Med Univ Lublin, Fac Pharm, Dept Pharmaceut Microbiol, PL-20093 Lublin, Poland

[3] Med Univ Lublin, Fac Pharm, Dept Organ Chem, PL-20093 Lublin, Poland

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2013年 / 10卷 / 09期

关键词：

Thiazoles; Thiosemicarbazones; Benzofuranone; Antimicrobial drugs; N-myristoyltransferase; Molecular modeling; FUNGAL N-MYRISTOYLTRANSFERASE; IN-VITRO ACTIVITY; ANTIFUNGAL AGENTS; CRYSTAL-STRUCTURE; CANDIDA-ALBICANS; 2-THIAZOLYLHYDRAZONE DERIVATIVES; BIOLOGICAL EVALUATION; ASYMMETRIC-SYNTHESIS; INHIBITORS; THIAZOLES;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 N-myristoyltransferase (NMT).

引用

页码：798 / 807

页数：10

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