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

被引：4

作者：

Varpe, Bhushan Dnyandeo ^{[1
]}

Jadhav, Shailaja Bhanudas ^{[1
]}

机构：

[1] Progress Educ Soc, Modern Coll Pharm, Pune 411044, Maharashtra, India

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICAL INVESTIGATION | 2021年 / 11卷 / 02期

关键词：

5-Fluoroisatin; Anti-inflammatory activity; Docking; Anti-tubercular activity; In silico ADME; ISATIN DERIVATIVES; PYRAZOLE; DESIGN; DRUG; THIOPHENE; ANTIBACTERIAL; DENATURATION; INFLAMMATION; ANTIFUNGAL; ARTHRITIS;

D O I：

10.5530/ijpi.2021.2.34

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 mu g/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.

引用

页码：189 / 194

页数：6

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