REPORT Insight into the lipophilicity of selected monosubstituted chalcones

Abstract

This study represents our attempt to understand how the antimicrobial activity of chalcones is modulated by their lipophilicity. To achieve this overall objective, a library of monosubstituted chalcones was targeted after careful consideration of the stereo electronic properties of the substituents appended in each of its constituent members. The lipophilicities of these derivatives were determined experimentally as well as by means of different validated computational programs. The theoretical determination was necessitated by the long-winded and time-consuming experimental protocols involved. It was gratifying to note the good correlation between these determinations which indicated the suitability of using such theoretical descriptors not only for assessing the lipophilicity of putative lead molecules but also for evaluating their biological activity. Standard disc diffusion technique employed against gram positive & negative bacteria as well as fungi revealed some preliminary information about the antimicrobial activity of these analogues.