2. Academic Validation
  3. Novel cajaninstilbene acid derivatives as antibacterial agents

Novel cajaninstilbene acid derivatives as antibacterial agents

  • Eur J Med Chem. 2015 Jul 15:100:235-45. doi: 10.1016/j.ejmech.2015.06.008.
Zhi-Zhong Geng 1,  Jian-Jun Zhang 1,  Jing Lin 2,  Mei-Yan Huang 1,  Lin-Kun An 3,  Hong-Bin Zhang 4,  Ping-Hua Sun 1,  Wen-Cai Ye 1,  Wei-Min Chen 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Jinan University, Guangzhou 510632, China.
  • 2 College of Pharmacy, Jinan University, Guangzhou 510632, China. Electronic address: linjing_jnu@163.com.
  • 3 School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
  • 4 Department of Clinical Laboratory, Guangzhou Liuhuaqiao Hospital, Guangzhou 510010, China.
  • 5 College of Pharmacy, Jinan University, Guangzhou 510632, China. Electronic address: twmchen@jnu.edu.cn.
PMID: 26093280 DOI: 10.1016/j.ejmech.2015.06.008
Abstract

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.

Keywords

Antibacterial; Cajaninstilbene acid; MRSA; Structure-activity relationship; Synthesis.

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