African Journal of
Pharmacy and Pharmacology

  • Abbreviation: Afr. J. Pharm. Pharmacol.
  • Language: English
  • ISSN: 1996-0816
  • DOI: 10.5897/AJPP
  • Start Year: 2007
  • Published Articles: 2285

Article in Press

Synthesis, Biological Evaluation and Molecular Modeling of Hybrid Compounds based on Different Fragments Clubbed with Pyrrole

Apeejay Stya University, Haryana

  •  Received: 03 August 2018
  •  Accepted: 03 August 2018
The limitations of currently available drugs and emergence of multidrug and extensively drug-resistant strains of Mycobacterium tuberculosis (Mtb) stress the need of new candidates as antitubercular agents. Different 2,5-dimethyl pyrrole derivatives clubbed with coumarin, naphthyl, furyl, phenyl, fragment of ibuprofen, fragment of diclofenac were synthesized and evaluated for antitubercular activity. The structure of all the derivatives synthesized was established on the basis of their spectral data. The compounds were tested against Mtb H37Rv (ATCC#27294) and resistant strain (INH, RIF and FQ resistant strains) by microplate alamar blue assay method and found to be active. The binding mode of these compounds was also studied by docking studies on InhA. The most potent compound 4t exhibited activity at 5.22 g/mL against the sensitive Mtb strain and was also found to be active against rifampicin resistant and floroquinoline resistant (RIF-R and FQ-R) strains at 9.45 and 12.2 g/mL.

Keywords: Pyrroles / Antitubercular activity / Synthesis / Assay