title: Synthesis and biological evaluation of 2-(3-fluoro-4-nitro phenoxy)-n-phenylacetamide derivatives as novel potential affordable antitubercular agents.
abstract: A novel series of 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide compounds were designed, synthesized and in vitro assessed for their antitubercular activities by a microdilution method. All the novel derivatives exerted potent or moderate active against M. tuberculosis H₃₇Rv, with MIC values ranging from 4 to 64 μg/mL. The most potent derivative 3m showed an identical MIC value of 4 μg/mL for both M. tuberculosis H₃₇Rv and rifampin-resistant M. tuberculosis 261. It demonstrated no inhibitory effects against six different tumor cell lines by a MTT assay and had a good safety profile in a vero cell line, providing a good lead for subsequent optimization in search of novel affordable antitubercular agents.
authors.affiliation: Key Laboratory of Drug Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Ang
authors.forename: Yan-Ni
authors.initials: YN
authors.lastname: Lin
authors.forename: Tao
authors.initials: T
authors.lastname: Yang
authors.forename: Jian-Zhong
authors.initials: JZ
authors.lastname: Yang
authors.forename: Wei-Yi
authors.initials: WY
authors.lastname: Pi
authors.forename: Ying-Hong
authors.initials: YH
authors.lastname: Yang
authors.forename: You-Fu
authors.initials: YF
authors.lastname: Luo
authors.forename: Yong
authors.initials: Y
authors.lastname: Deng
authors.forename: Yu-Quan
authors.initials: YQ
authors.lastname: Wei
mesh_terms: D000083:Acetanilides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002522:Chlorocebus aethiops; D045325:HCT116 Cells; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D012293:Rifampin / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000083:Acetanilides; D000995:Antitubercular Agents; D012293:Rifampin