Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 7, Pages 2815-2821Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.12.021
Keywords
1,5-Benzothiazepine; Synthesis; Biological evaluation; Antimicrobial agent
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Funding
- National Natural Science Foundation of China [20772021]
- Natural Science Foundation of Hebei Province, China [2007000239]
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Two series of novel 1,5-benzothiazepine derivatives (23 compounds) were efficiently synthesized and evaluated for antibacterial and antifungal activities. The results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms and showed higher activity against fungi than bacteria. Compound 2e exhibited the greatest antimicrobial activity. Preliminary study of the structure-activity relationship revealed that substituents in phenyl rings had a great effect on the antimicrobial activity of these compounds. (C) 2008 Published by Elsevier Masson SAS.
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