Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 100, Issue -, Pages 235-245Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.06.008
Keywords
Cajaninstilbene acid; Synthesis; Antibacterial; MRSA; Structure-activity relationship
Categories
Funding
- Natural Science Foundation of Guangdong Province [2014A030311021]
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Discovery of novel antibacterial agents with new structural scaffolds that combat drug-resistant pathogens is an urgent task. Cajaninstilbene acid, which is isolated from pigeonpea leaves, has shown antibacterial activity. In this study, a series of cajaninstilbene acid derivatives were designed and synthesized. The antibacterial activities of these compounds against gram-negative and gram-positive bacteria, as well as nine strains of methicillin-resistant staphylococcus aureus (MRSA) bacteria are evaluated, and the related structure-activity relationships are discussed. Assays suggest that some of the synthetic cajaninstilbene acid derivatives exhibit potent antibacterial activity against gram-positive bacterial strains and MRSA. Among these compounds, 5b, 5c, 5j and 5k show better antibacterial activity than the positive control compounds. The results of MTT assays illustrate the low cytotoxicity of the active compounds. (C) 2015 Elsevier Masson SAS. All rights reserved.
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