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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

1★, 1★ Corresponding author

  1. 1Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA.

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Bhushan Dnyandeo Varpe

Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA.

bhushanvarpe@outlook.com

Received: 05-05-2021; Revised: 21-05-2021; Accepted: 20-06-2021.

Volume 11, Issue 2 · pp. 189-194 · 2021 · DOI: 10.5530/ijpi.2021.2.34

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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    Varpe, B. D., & Jadhav, S. B. (2021). 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. International Journal of Pharmaceutical Investigation, 11(2), 189-194. https://doi.org/10.5530/ijpi.2021.2.34

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    © 2021 Author(s)

    This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms. CC BY-NC-SA 4.0