title: Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives.
abstract: The synthesis of (S)-2-(4-tert-butylphenoxy)-3-(benzoxazol-5-yl) propanoic acid derivatives (2a-k) were described and their in vitro antibacterial activities were determined against Gram-negative and -positive bacteria. These compounds were found to exert a broad spectrum of activity against the screened bacteria, but poor MIC values were found for Candida albicans fungi. Compound 2b bearing a hydrophobic aromatic tie was the most active derivative against all bacteria studied with MIC values ranging from 0.098 to 0.78 μg/mL. The activity of 2b against B. subtilis was 2-fold higher than Penicillin, and 8- to 510-fold higher than other control antibiotics.
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China; Department of Chemistry, University of Florida, Gainesville, FL, 32611-7200, USA.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Jingbao
authors.initials: J
authors.lastname: Liu
authors.affiliation: Department of Chemistry, University of Florida, Gainesville, FL, 32611-7200, USA.
authors.forename: Jocelyn M
authors.initials: JM
authors.lastname: Macho
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Xizhen
authors.initials: X
authors.lastname: Jiang
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Dongsheng
authors.initials: D
authors.lastname: Xie
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China.
authors.forename: Faqin
authors.initials: F
authors.lastname: Jiang
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: sdwenlu@sjtu.edu.cn.
authors.forename: Wenlu
authors.initials: W
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd., Shanghai 200240, China. Electronic address: leifu@sjtu.edu.cn.
authors.forename: Lei
authors.initials: L
authors.lastname: Fu
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D008826:Microbial Sensitivity Tests
chemical_list: D000890:Anti-Infective Agents; D001583:Benzoxazoles
keywords: Antibacterial activity; Benzoxazole; Minimum inhibitory concentration; Propanoic acid