title: Design, synthesis and antibacterial evaluation of novel AHL analogues.
abstract: Two series of novel AHL analogues were designed, synthesized and evaluated for antibacterial activity under cell membrane conditions in vitro. Analogues 4a-c and 4g-m presented potent activity against Gram-positive bacteria. Especially the analogue 4l exerted the most potent inhibition against Bacillus subtilis with MIC50 value of 1.443μg/ml. To our surprise, analogues 6a-c and 6g showed weak inhibition against Gram-negative bacteria with MIC50 values ranging from 17.589 to 67.840μg/ml. This was the first report about synthesis and antibacterial evaluation in vitro of AHL analogues containing dithioester linkage.
authors.affiliation: School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Jing-Li
authors.initials: JL
authors.lastname: Ren
authors.forename: En
authors.initials: E
authors.lastname: Zhang
authors.forename: Xian-Wei
authors.initials: XW
authors.lastname: Ye
authors.forename: Meng-Meng
authors.initials: MM
authors.lastname: Wang
authors.forename: Bin
authors.initials: B
authors.lastname: Yu
authors.forename: Wen-Hua
authors.initials: WH
authors.lastname: Wang
authors.forename: Ya-Zhuo
authors.initials: YZ
authors.lastname: Guo
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002219:Carbamates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D053038:Quorum Sensing / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D002219:Carbamates; C088386:homoserine lactone; D015107:4-Butyrolactone