title: Synthesis of 1-isopropyl-3-acyl-5-methyl-benzimidazolone derivatives and their antimicrobial activity.
abstract: A series of N-acylated analogues of 1-isopropyl-3-acyl-5-methyl-benzimidazolone were synthesized. Bioassay results indicated that analogues 5-07 and 5-19 exhibited the most potency against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Analogues 5-02, 5-07, 5-12, 5-15, 5-19, 5-20 and 5-25 could effectively inhibit the spore germination of Botrytis cinerea. The relationship between structure and their antimicrobial activity (SAR) has also been discussed according to aliphatic acids and aromatic acids derivatives, respectively. This implied that the N-acylated derivatives of 5-methyl-benzimidazolone might be potential antimicrobial agents.
authors.affiliation: College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China. jizhiqin@nwsuaf.edu.cn.
authors.forename: Nan
authors.initials: N
authors.lastname: Xu
authors.forename: Chunnan
authors.initials: C
authors.lastname: Yang
authors.forename: Xinqi
authors.initials: X
authors.lastname: Gan
authors.forename: Shaopeng
authors.initials: S
authors.lastname: Wei
authors.forename: Zhiqin
authors.initials: Z
authors.lastname: Ji
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020171:Botrytis / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013172:Spores, Fungal / Q000187:drug effects / Q000254:growth & development
chemical_list: D000890:Anti-Infective Agents; D001562:Benzimidazoles; C014353:benzimidazolone