Successively Substituting an Additional
4-(2-Aminoethyl) Aniline Group in Fabricated
Isoindoline-1,3-Dione Scaffold Enhances the
Antimicrobial Potency: Part II of Research
Volume 2 - Issue 2
Debarshi Kar Mahapatra1*, Mohamad Taleuzzaman2, Santosh S Chhajed3
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- 1Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, India
- 2Department of Pharmaceutical Chemistry, Glocal School of Pharmacy, Glocal University, India
- 3Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, India
*Corresponding author:
Debarshi Kar Mahapatra, Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of
Pharmacy, Nagpur 440037, Maharashtra, India
Received: August 11, 2018; Published: August 21, 2018
DOI: 10.32474/DDIPIJ.2018.02.000132
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Abstract
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.
Keywords: Antimicrobial; Antifungal; Antibacterial; Phthalimide; Isoindoline; Synthesis
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