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喹啉衍生物的抗菌和遗传毒性特性。

Antimicrobial and genotoxic properties of quinoline derivatives.

作者信息

Zani F, Carmellino M L

机构信息

Dipartimento Farmaceutico, Università di Parma, Italy.

出版信息

Boll Chim Farm. 1994 May;133(5):328-38.

PMID:8068239
Abstract

We continued our research into the biological properties of quinoline derivatives. Newly synthesized 8-sulfonylquinolines, tested against some representative microbial strains and practically inactive, were also studied for the genotoxic properties. The genotoxicity tests were extended to previously synthesized compounds (some 6-substituted 8-quinolinecarboxylic acids, the amide and some esters of 8-quinolinecarboxylic acid and finally the 8-quinolinecarboxaldehyde and two of its derivatives). Rec-assay and Salmonella-microsome tests showed several compounds to be genotoxic; the mutagenic activity seems to be modulated by the nature of the substituents. The results obtained are discussed with the aim of explaining possible structure-activity relationships.

摘要

我们继续对喹啉衍生物的生物学特性进行研究。新合成的8-磺酰基喹啉针对一些代表性微生物菌株进行了测试,结果显示其实际无活性,同时也对其遗传毒性特性进行了研究。遗传毒性测试扩展到了先前合成的化合物(一些6-取代的8-喹啉羧酸、8-喹啉羧酸的酰胺和一些酯,以及最终的8-喹啉甲醛及其两种衍生物)。重组分析和沙门氏菌-微粒体测试表明,有几种化合物具有遗传毒性;诱变活性似乎受取代基性质的调节。对所得结果进行了讨论,旨在解释可能的构效关系。

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