Microwave Assisted, Solvent-Free, 'Green' Synthesis of Novel Indole Analogs as Potent Antitubercular and Antimicrobial Agents and Their Molecular Docking Studies
| Autor: | A. S. Rathod, J. S. Biradar, S. S. Godipurge |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Indole test
biology 010405 organic chemistry INHA Protein Data Bank (RCSB PDB) Active site General Chemistry 010402 general chemistry Coumarin Antimicrobial 01 natural sciences Combinatorial chemistry 0104 chemical sciences chemistry.chemical_compound chemistry Docking (molecular) biology.protein Structure–activity relationship |
| Zdroj: | Russian Journal of General Chemistry. 88:1238-1246 |
| ISSN: | 1608-3350 1070-3632 |
| DOI: | 10.1134/s1070363218060324 |
| Popis: | A rapid, efficient and environmentally benign synthesis of novel indole analogs bearing thiazolidinone attached to substituted thiazolyl coumarin scaffolds are synthesized. Conventional and microwave-assisted (MW) approaches are studied. Structures of the products are confirmed by FT-IR, NMR (1H and 13C) and Mass spectra. The in vitro antitubercular and antimicrobial activities are evaluated. Several screened compounds demonstrate promising anti-TB and antimicrobial properties. The structure activity relationship (SAR) study reveal that the compounds containing halogens are most potent. Docking of the potent compounds inside the active site of a target enzyme mycobacterial enoyl reductase (InhA)(PDB code 4TZK) is performed. |
| Databáze: | OpenAIRE |
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