Abstract
A series of C-(3-aminomethyl-cyclohexyl)-methylamine derivatives were synthesized and evaluated for their antitubercular activity. Some of the compounds exhibited potent activity against Mycobacterium tuberculosis H37Rv. One of the compound having t-butyl at para position of the benzene ring showed excellent activity even better than the standard drug ethambutol with MIC value 1.1±0.2μM. The time-kill kinetics study of two most active compounds showed rapid killing of the M. tuberculosis within 4days. Additionally atom-based quantitative structure–activity relationship (QSAR) model was developed that gave a statistically satisfying result (R2)=0.92, Q2=0.75, Pearson-R=0.96 and effectively predicts the anti-tuberculosis activity of training and test set compounds.
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