Sheela, K. and Santhosh, C. and Singh, Krishna Ravi and Sharath, K. and Sadashiva, M. P. (2024) An efficient synthesis of mono-, di-, and tri-substituted 1,3-thiazoles employing functionalized thioamides as thiocarbonyl precursors. Organic & Biomolecular Chemistry, 22 (17). pp. 3490-3501.
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Herein, we report an efficient strategy to synthesize functionalized 1,3-thiazoles using alkyl 2-amino-2-thioxoacetates. Thioamides, the synthetic precursors, react effortlessly with electrophilic reagents and are transformed into a series of phenyl-, methyl-, and acyl-substituted thiazoles with high functionalization at the 2nd position through sequential C–S/C–N bond formation. Rapid reaction times under metal-free mild conditions is a noteworthy feature of the reported protocol. Given the intriguing biological significance of the synthesized molecules, we further performed a comprehensive evaluation of their potency against the SARS-CoV-2 receptor (PDB ID: 7mc6) using a molecular docking approach, with binding scores ranging from −4.3 to −8.2 kcal mol−1.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Aqueous-Phase Synthesis facile Synthesis thiazolederivatives cyclizationoxazole, metal, acid2- Aminothiazoles, aminothiazoles |
| Subjects: | C Chemical Science > Organic Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | C Swapna Library Assistant |
| Date Deposited: | 18 Oct 2025 09:54 |
| Last Modified: | 18 Oct 2025 09:54 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/17859 |
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