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含噻吩、呋喃和喹啉部分的杂环查尔酮衍生物的合成及抑菌活性。

Synthesis and anti-bacterial activity of some heterocyclic chalcone derivatives bearing thiofuran, furan, and quinoline moieties.

机构信息

Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji, P.R. China.

出版信息

Arch Pharm (Weinheim). 2011 Oct;344(10):689-95. doi: 10.1002/ardp.201100005. Epub 2011 Sep 2.

Abstract

36 Novel heterocyclic chalcone derivatives were synthesized and tested for their anti-bacterial activity. Some compounds presented good anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Streptococcus mutans, among which the derivatives F2 with an MIC of 2 µg/mL was as active as the standard drug (norfloxacin) and less active than oxacillin. All the compounds did not inhibit the growth of Gram-negative bacteria (Escherichia coli CCARM 1924 or Escherichia coli CCARM 1356) at 64 µg/mL.

摘要

合成了 36 种新型杂环查尔酮衍生物,并测试了它们的抗菌活性。一些化合物对革兰氏阳性菌(包括多药耐药的临床分离株)表现出良好的抗菌活性。这一类化合物对变异链球菌具有很高的活性,其中衍生物 F2 的 MIC 为 2μg/ml,与标准药物(诺氟沙星)活性相当,低于苯唑西林。所有化合物在 64μg/ml 时均不抑制革兰氏阴性菌(大肠杆菌 CCARM 1924 或大肠杆菌 CCARM 1356)的生长。

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