International Journal of Pharmaceutical Investigation, 2021, 11, 2, 189-194.
DOI: 10.5530/ijpi.2021.2.34
Published: July 2021
Type: Original Article
Authors:
Bhushan Dnyandeo Varpe
Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA
Shailaja Bhanudas Jadhav
Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA
ABSTRACT
Objectives: To synthesize Schiff base conjugate of 5-Fluoroisatin with thiophene- 2-ethylamine and its Mannich bases and screen for anti-inflammatory and anti-tubercular activity. Materials and Methods: The compounds were synthesized by Schiff and Mannich base reactions. The anti-inflammatory activity was studied by analyzing the percentage inhibition of denaturation of Bovine Serum Albumin and anti-tubercular activity using the Almar blue assay against Mycobacterium tuberculosis (MTB H37Rv). To understand the interactions of compounds with receptors and pharmacokinetic properties, in silico studies were performed. Results: The compound ITF 5 (80.08%) showed good anti-inflammatory activity. Also, compound ITF 5 (MIC: 6.25 μg/ml) was found most active against MTB H37Rv (ATCC-27294). Conclusion: Compounds showed good anti-inflammatory activities and relatively weak anti-tubercular activities as compared to standards. The compounds ITF 5 with N-phenylpiperazine containing Mannich base showed better anti-inflammatory and anti-tubercular activity as compared to other compounds.
Keywords: 5-Fluoroisatin, Anti-inflammatory activity, Docking, Anti-tubercular activity, In silico ADME.