| Novel synthetic approaches targeting therapeutically active agents |
| Paper ID : 1007-ISCH |
| Authors |
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Reham A. Mohamed-Ezzat *1, Galal H. Elgemeie2 1Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Center, Cairo, Egypt. 2Department of Chemistry, Faculty of Science, Helwan University, Helwan, Cairo, Egypt. |
| Abstract |
| New strategies targeting the synthesis of novel triazine sulfonamides as potent antiviral agents have been accomplished via reacting the sulfaguanidine derivatives with N-cyanodithioiminocarbonate. Further reaction of the new triazine sulfonamides with various secondary amines furnished several substituted triazine sulfonamide derivatives of promising broad-spectrum activities. New class of triazine sulfonamide thioglycosides was also designed and synthesized. The new structures were generated via a direct approach starting from potassium cyanocarbonimidodithioate, then the corresponding triazine sulfonamide thioglycosides were generated. Characterizations of the compounds have been determined utilizing NMR spectroscopy and single crystal X-ray diffraction technique. The anti-viral activity of the compounds against SARS CoV-2 virus was investigated utilizing MTT cytotoxicity assay to estimate the half-maximal cytotoxic concentration (CC50) and inhibitory concentration 50 (IC50). The most active compound demonstrated potent anti-viral potency against SARS-CoV-2 with IC50 = 2.378 µM as compared to the activity of the anti-viral drug remdesivir (IC50 = 10.11 µM). Anti-viral investigations of the triazine sulfonamide thioglycosides in vitro against HCoV-229E virus revealed that some compounds possess promising activity. Some compounds indicated moderate anti-viral activity against low pathogenic coronavirus 229E as compared to remdesivir at a concentration of 100 μg/mL. Our results demonstrate that these novel triazine sulfonamides could potentially serve as new anti-viral drugs. |
| Keywords |
| Synthesis, Triazines, Sulfonamides, Thioglycosides, SARS‑CoV‑2, HCoV-229E. |
| Status: Abstract Accepted (Oral Presentation) |