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Z Naturforsch C. 2018 Feb 23;73(3-4):117-122. doi: 10.1515/znc-2017-0063.

Design, synthesis, and antibacterial activity of novel 8-methoxyquinoline-2-carboxamide compounds containing 1,3,4-thiadiazole moiety.

Author information

1
Key Laboratory at University of Education Department of Xinjiang Uygur Autonomous Region, Yili Normal University, Yining 835000, P.R. China.
2
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, Henan Province, P.R. China.
3
Xingping Food and Drug Administration, Xingping 713100, Shaanxi Province, P.R. China.
4
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, Henan Province, P.R. China, Phone/Fax: +86 371 67781912.

Abstract

A series of novel 8-methoxyquinoline-2-carboxamide compounds containing 1,3,4-thiadiazole moiety was designed and synthesized by using an active substructure combination method. Then, the antibacterial activities of all the target compounds were evaluated in vitro against three Gram-positive bacteria and three Gram-negative bacteria. The antibacterial assay showed that some target compounds displayed moderate to good antibacterial efficacy in comparison with the reference drug Chloromycin. Some interesting results of structure-activity relationships were also discussed.

KEYWORDS:

1,3,4-thiadiazole; 2-methyl-8-hydroxyquinoline; antibacterial activity; structure-activity relationships

PMID:
28753551
DOI:
10.1515/znc-2017-0063

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