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Synthesis and in vitro anti Mycobacterium tuberculosis activity of a series of phthalimide derivatives.

Bioorganic & medicinal chemistry (2009-05-12)
Jean L Santos, Paulo R Yamasaki, Chung Man Chin, Célio H Takashi, Fernando R Pavan, Clarice Q F Leite
ABSTRACT

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.

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Sigma-Aldrich
Phthalimide, ≥99%
Sigma-Aldrich
Phthalimide potassium salt, 98%
Supelco
Isoniazide, analytical standard, ≥99% (TLC)
Sigma-Aldrich
Phthalimide potassium salt, purum, ≥99.0% (NT)