Synthesis and Antimicrobial Activities of (4,5,6,7-Tetrahydro-1H-indazol-2(3H)-yl)thiazole Derivatives

被引：6

作者：

Laczkowski, Krzysztof Z. ^{[1
]}

Misiura, Konrad ^{[1
]}

Biernasiuk, Anna ^{[2
]}

Malm, Anna ^{[2
]}

机构：

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

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

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2014年 / 11卷 / 08期

关键词：

Antibacterial drugs; Antifungal drugs; Candida spp; Tetrahydroindazole; Thiazole; IN-VITRO ACTIVITY; 2,4-DISUBSTITUTED THIAZOLES; ANTIPROLIFERATIVE ACTIVITY; PHARMACOLOGICAL EVALUATION; BIOLOGICAL-ACTIVITY; ACID; ANTIBACTERIAL; CYTOTOXICITY; INHIBITORS; DESIGN;

D O I：

10.2174/1570180811666140516233913

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis, characterization and investigation of antimicrobial activities of ten novel tetrahydroindazolyl-thiazoles is presented. Their structures were determined using H-1 and C-13 NMR, FAB(+)-MS and HRMS analyses. Among the derivatives, compound 3f shows strong antibacterial activity against S. aureus ATCC 43300, S. aureus ATCC 25923, and S. epidermidis ATCC 12228 with MIC 7.81 mu g/ml, and good activity against S. aureus ATCC 6538 with MIC 31.25 mu g/ml. Compounds 3a-e and 3j show good antifungal activity with MIC values ranging from 31.25 mu g/ml to 250 mu g/ml.

引用

页码：960 / 967

页数：8

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