Original ArticleInternational Journal of Pharmaceutical InvestigationVol. 11 | Issue 2 | 2021 | pp. 189–194Open access
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
- 1 Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA.
Published in International Journal of Pharmaceutical Investigation
Correspondence: Bhushan Dnyandeo Varpe
Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA.
Email: bhushanvarpe@outlook.com
Copyright: © 2021 Manuscript Technomedia. This is an open access article.
- Published:
- Jul 1, 2021
- Received:
- May 5, 2021
- Accepted:
- Jun 20, 2021
How to cite
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
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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Article metadata
| Title | 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 |
|---|---|
| Authors | Bhushan Dnyandeo Varpe; Shailaja Bhanudas Jadhav |
| Affiliations | Progressive Education Society’s, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA. |
| Corresponding author | bhushanvarpe@outlook.com |
| Journal | International Journal of Pharmaceutical Investigation |
| Volume / Issue | Vol. 11, Issue 2 (2021) |
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