The
irrational use of antimicrobial agents for several decades has led to the
drug-resistance among the patient population. Overcoming the present
drug-resistance is a major challenge for modern day scientists. In order to
counter this problem, several approaches have been utilized, one of which
involve drug design and discovery, where new classes or unexplored chemical
moieties are explored for a particular activity, either serendipitously or
quite rationally. Learning lessons from the previously synthesized four compounds
(Part-I of Research), we have now (Part-II of Research) designed two compounds
(3 and 5) by incorporating an additional 4-(2-aminoethyl)aniline group in the
fabricated isoindoline-1,3-dione scaffold by successive synthetic step
utilizing similar protocol and screened them against the above four mentioned
pathogenic microbes in a similar way. The present exploration is an attempt to rationally
overcome the microbial drug resistance by the efficacious and potent nature of
the compounds. Compound (5) exhibited the highest activity against A. niger with
ZOI diameter of >29mm. All the compounds showed more or less nearly the same
activity. From this study, it may be concluded that substituting the
amine/amide-based components leads to an increase in the potency of the
compared along with better-anti-fungal activity. Therefore, the current
exploration helped to design the compounds which have better potency than our
previous reports and also providing imperative knowledge regarding the
selection of the substituents. The encouraging results will further motivate us
in developing novel and better inhibitors of phthalimide scaffold in the
future.
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