In a quest for developing novel anti-tubercular agents, a series of 3-benzylidene-4-chromanones 1a-l were evaluated for growth inhibition of Mycobacterium tuberculosis H37Rv. Three promising compounds 1d, g, j emerged as the lead compounds with the IC50 and IC90 values of less than 1μg/mL. Evaluation of the potent compounds 1d, g, j and k against Vero monkey kidney cells revealed that these compounds are far more toxic to M. tuberculosis than to Vero cells. Structure-activity relationships demonstrated that 3-benzylidene-4-chromanones are more potent against M. tuberculosis than the related 2-benzylidene cycloalkanones and the meta substituted chromanone derivatives are more active than their ortho-and para-counterparts. Some guidelines for amplifying the project are presented.
|Number of pages||5|
|Journal||Journal of enzyme inhibition and medicinal chemistry|
|Publication status||Published - Apr 1 2015|
- Structure-activity relationships
- Unsaturated ketones
ASJC Scopus subject areas
- Drug Discovery