title: Novel cajaninstilbene acid derivatives as antibacterial agents.
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.
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China.
authors.forename: Zhi-Zhong
authors.initials: ZZ
authors.lastname: Geng
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China.
authors.forename: Jian-Jun
authors.initials: JJ
authors.lastname: Zhang
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China. Electronic address: linjing_jnu@163.com.
authors.forename: Jing
authors.initials: J
authors.lastname: Lin
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China.
authors.forename: Mei-Yan
authors.initials: MY
authors.lastname: Huang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
authors.forename: Lin-Kun
authors.initials: LK
authors.lastname: An
authors.affiliation: Department of Clinical Laboratory, Guangzhou Liuhuaqiao Hospital, Guangzhou 510010, China.
authors.forename: Hong-Bin
authors.initials: HB
authors.lastname: Zhang
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China.
authors.forename: Ping-Hua
authors.initials: PH
authors.lastname: Sun
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China.
authors.forename: Wen-Cai
authors.initials: WC
authors.lastname: Ye
authors.affiliation: College of Pharmacy, Jinan University, Guangzhou 510632, China. Electronic address: twmchen@jnu.edu.cn.
authors.forename: Wei-Min
authors.initials: WM
authors.lastname: Chen
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D012459:Salicylates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C549543:3-hydroxy-4-prenyl-5-methoxystilbene-2-carboxylic acid; D000900:Anti-Bacterial Agents; D012459:Salicylates; D013267:Stilbenes
keywords: Antibacterial; Cajaninstilbene acid; MRSA; Structure-activity relationship; Synthesis