Antimycobacterial activity of 5-arylidene derivatives of hydantoin

Abstract

The synthesis of various 5-arylidene-2-thiohydantoins and results of the primary assay in vitro for their antimycobacterial activity is reported. Eight of those compounds exhibited > 90% inhibition of Mycobacterium tuberculosis growth and for them the minimum inhibitory concentrations, cytotoxicity (IC50) and the selectivity index values were determined. The most active structure, (5Z)-5-(1,1'-biphenyl-4-ylmethylene)-2-thioxoimidazolidin-4-one, showed MIC = 0.78 microg/ml. For all compounds log P and log D (pH 6.5) values were calculated.