Synthesis of new benzenesulfonamide and benzisothiazolone derivatives as proteolytic enzyme inhibitors
Mansoura Journal of Pharmaceutical Sciences. 2004; 20 (1): 22-33
in English
| IMEMR
| ID: emr-200426
ABSTRACT
Starting from saccharin sodium, two types of the hydrazide derivatives, 3 and 11 were prepared which underwent condensation with different aromatic aldehydes to give the hydrazone derivatives 4 and 12, respectively. Moreover, the hydrazide 3 was cyclized using CS[2] in ethanolic KOH solution to afford the oxadiazole derivative 5. Reaction of the oxadiazole 5 with methyl iodide in ethanolic KOH at room temperature gave the corresponding thioether derivative 6. The thiosemicarbazide 7 was obtained in high yield by the reaction of the hydrazide 3 and phenyl isothiocyanate at room temperature which was cyclized either in basic media to afford the triazole derivative 8 or under acidic condition to give the thiadiazole 9. Most novel compounds have been examined for their proteolytic enzyme inhibitory activity whereas compounds 6, 9 and 12h showed the highest inhibitory activity
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Index:
IMEMR (Eastern Mediterranean)
Language:
English
Journal:
Mansoura J. Pharm. Sci.
Year:
2004
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