Sat, 16 Dec 2017

Design, Synthesis, Characterization and Biological Evaluation of some novel Heterocyclic derivatives as Anti-Tubercular agents

Ayyadurai Jerad Suresh*1, Parakkot Ramakrishnan Surya1, Antonyraj Velankani1

1. Department of pharmaceutical chemistry, College of Pharmacy, Madras Medical College, Chennai-600003, India


ABSTRACT

Tuberculosis is a serious threat to public health throughout the world. Schiff bases are compounds carrying the imine or azomethine (–C=N–) functional group. Recent studies report that benzimidazole based Schiff bases possess antibacterial, antimicrobial, anti-tubercular, and anti-inflammatory activities. 1,2 Further it has been known that fluoroaniline moiety can have profound and unexpected results in biological activity 19. A series of benzimidazole and fluroaniline based Schiff bases were designed and docked against crucial mtb enzyme target Glutamine synthetase1. The molecules with good docking-score and multiple interactions were chosen for synthesis. Compounds (BE1, BE2, FA-1, FA-2, and FA-3) were synthesized by reflux condensation reaction with good yield. The newly synthesized compounds were characterized by spectral methods and evaluated for anti- mycobacterial activity against tuberculosis H37RV strain. Anti-tubercular activity was carried out by using Microplate Alamar Blue Assay (MABA) method. The experimental results revealed that Compounds (BE1& BE2) showed promising anti-tubercular activity with an MIC below 0.8 mcg/mL while (FA-1, FA-2, and FA-3) showed moderate anti tubercular activity with an MIC below 6.25 and 12.5 mcg/mL.

Key words: Benzimidazole, Schiff base, Fluoroaniline, Docking, Anti-tubercular.


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