1. One-pot synthesis of sulfonyl-1H-1,2,3-triazolyl-thiomorpholine 1,1-dioxide derivatives and evaluation of their biological activity
- Author
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N. Vasudeva Reddy, Mettu Ravinder, Rakesh Sreerama, T Narasimha Swamy, and Sirassu Narsimha
- Subjects
Sulfonyl ,chemistry.chemical_classification ,1,2,3-Triazole ,010405 organic chemistry ,Organic Chemistry ,One-pot synthesis ,Biological activity ,010402 general chemistry ,01 natural sciences ,Biochemistry ,0104 chemical sciences ,Inorganic Chemistry ,chemistry.chemical_compound ,Thiomorpholine ,chemistry ,Organic chemistry ,Antibacterial activity - Abstract
A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (5a–5l) in good yields (63 to 77%) using different sulfonic acids and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide through the in situ generated sulfonyl azides was developed. The structures of the newly synthesized compounds were confirmed by 1H NMR, 13C NMR, mass spectrometry, and elemental analysis. The newly synthesized compounds were screened for in vitro antibacterial activity and free radical scavenging activity in terms of hydrogen donating or radical scavenging ability by the DPPH method. Among all, the compound N-(4-((4-((1,1-dioxidothiomorpholino) methyl)-1H-1,2,3-triazol-1-yl)sulfonyl)phenyl) acetamide (5l) was found to exhibit potent activity as compared to the standard drugs.
- Published
- 2020