title: Synthesis and antibacterial activity of 3-benzylamide derivatives as FtsZ inhibitors.
abstract: The emergence and spread of multidrug-resistant strains of the human pathological bacteria are generating a threat to public health worldwide. In the current study, a series of PC190723 derivatives was synthesized and investigated for their antimicrobial activity. The compounds exhibited good activity against several Gram-positive bacteria as determined by comparison of diameters of the zone of inhibition of test compounds and standard antibiotics. Compound 9 with a fluorine substitution on the phenyl ring showed the best antibacterial activity in the series against M. smegmatis with the zone ratio of 0.62, and against S. aureus with the zone ratio of 0.44. The results from this study indicate that based on the unique 3-methoxybenzamide pharmacophore, compound 9 may represent a promising lead candidate against Gram-positive bacteria that are worthy of further investigation.
authors.affiliation: School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, Hubei, China.
authors.forename: Zhongping
authors.initials: Z
authors.lastname: Hu
authors.affiliation: School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, Hubei, China.
authors.forename: Shasha
authors.initials: S
authors.lastname: Zhang
authors.affiliation: State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, Shanghai Institute of Pharmaceutical Industry, State Institute of Pharmaceutical Industry, Shanghai 200437, China.
authors.forename: Weicheng
authors.initials: W
authors.lastname: Zhou
authors.affiliation: School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, Hubei, China. Electronic address: xiangma@hust.edu.cn.
authors.forename: Xiang
authors.initials: X
authors.lastname: Ma
authors.affiliation: School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, Hubei, China. Electronic address: gyxiang1968@hotmail.com.
authors.forename: Guangya
authors.initials: G
authors.lastname: Xiang
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D006801:Humans; D020102:Mycobacterium smegmatis / Q000187:drug effects; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D001549:Benzamides; C531944:PC190723; D011725:Pyridines; D013844:Thiazoles; C025159:3-methoxybenzamide
keywords: 3-Methoxybenzamide; Antibacterial agents; FtsZ; Mycobacterium tuberculosis; Staphylococcus aureus