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新型氟喹诺酮衍生物的合成及体外抗菌活性评价。

Synthesis and in vitro antimicrobial evaluation of novel fluoroquinolone derivatives.

机构信息

Department of Industrial Chemistry, Alagappa University, Karaikudi-630 003, Tamil Nadu, India.

出版信息

Eur J Med Chem. 2010 Dec;45(12):6101-5. doi: 10.1016/j.ejmech.2010.09.036. Epub 2010 Sep 22.

Abstract

A series of 1-ethyl-6,8-difluoro-4-oxo-7(4-aryl piperazin-1-yl) 1,4-dihydro-quinoline-3-carboxylic acid derivatives (6a-f) and 1-ethyl-6,8-difluoro-4-oxo-7(4-piperidin-1-yl) 1,4-dihydro-quinoline-3-carboxylic acid derivatives (7a-e) were synthesized and evaluated for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by the microbroth dilution technique. The compounds were also evaluated for antifungal activity against Candida albicans (ATCC 90028) and Cryptococcous neoformans (ATCC 14116) pathogens. The preliminary in vitro evaluation studies revealed that some of the compounds have promising antimicrobial activities.

摘要

一系列 1-乙基-6,8-二氟-4-氧代-7(4-芳基哌嗪-1-基)-1,4-二氢喹啉-3-羧酸衍生物(6a-f)和 1-乙基-6,8-二氟-4-氧代-7(4-哌啶-1-基)-1,4-二氢喹啉-3-羧酸衍生物(7a-e)被合成并评估了其抗菌和抗真菌活性。采用微量肉汤稀释法评估化合物的抗菌活性。还评估了化合物对白色念珠菌(ATCC 90028)和新型隐球菌(ATCC 14116)病原体的抗真菌活性。初步的体外评价研究表明,一些化合物具有有前景的抗菌活性。

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