Schiff Base Conjugate of 5-Fluoroisatin with Thiophene-2-Ethylamine and its Mannich Bases: Synthesis, Molecular Docking, and Evaluation of in vitro Anti-inflammatory and Anti-tubercular Activity

  • 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
Keywords: 5-Fluoroisatin, Anti-inflammatory activity, Docking, Anti-tubercular activity, In silico ADME

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.

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Author Biography

Shailaja Bhanudas Jadhav, Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA
 
Docking pose and 2D interaction diagram of ITF 7
Published
2021-07-16
How to Cite
1.
Varpe BD, Jadhav SB. Schiff Base Conjugate of 5-Fluoroisatin with Thiophene-2-Ethylamine and its Mannich Bases: Synthesis, Molecular Docking, and Evaluation of in vitro Anti-inflammatory and Anti-tubercular Activity. ijpi [Internet]. 16Jul.2021 [cited 2Aug.2021];11(2):189-94. Available from: https://jpionline.org/index.php/ijpi/article/view/1027