Synthesis and in vitro anti Mycobacterium tuberculosis activity of a series of phthalimide derivatives.
New phthalimide derivatives were easily prepared through condensation of phthalic anhydride and selected amines with variable yields (70-90%). All compounds (3a-l) were evaluated against Mycobacterium tuberculosis H(37)Rv using Alamar Blue susceptibility. The compounds 3c, 3i, and 3l have the minimum inhibitory concentrations (MICs) of 3.9, 7.8, and 5.0 microg/mL, respectively, and could be considered new lead compounds in the treatment of tuberculosis and multi-drug resistant tuberculosis.
Lapdesf-Laboratório de Pesquisa e Desenvolvimento de Fármacos, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista Júlio de Mesquita Filho, Araraquara, SP, Brazil. jeanleandrosantos@yahoo.com.br
Jean L
JL
Santos
Paulo R
PR
Yamasaki
Chung Man
CM
Chin
Célio H
CH
Takashi
Fernando R
FR
Pavan
Clarice Q F
CQ
Leite
D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010797:Phthalimides / Q000737:chemistry*
D000995:Antitubercular Agents; D010797:Phthalimides; C037431:phthalimide