Synthesis and Some Pharmacological Studies of New Benzenesulfonamide Derivatives |
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| Authors: | Eatedal H Abdel Aal Osama I El-Sabbagh Shaker Youssif Sameh M El-Nabtity |
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| Institution: | (1) Departments of Pharmaceutical, Organic, and Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt, EG;(2) Department of Chemistry, Faculty of Science, Zagazig University, Zagazig, Egypt, EG;(3) Department of Pharmacology, Faculty of Veterinary Medicine, Zagazig University, Zagazig, Egypt, EG |
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| Abstract: | Summary. New benzenesulfonamide derivatives containing pyrazole and oxadiazole moieties were prepared starting from sodium saccharin.
The structures of the novel compounds were characterized by elemental analyses and spectroscopic methods. The new compounds
are structurally related to the COX-2 inhibitor celecoxib (Celebrex?). A pharmacological study of the pyrazoles revealed that several compounds possess higher analgesic and antiinflammatory
activities than celecoxib, particularly 11 and 17. Most of the pyrazoles showed a significant increase in the sleeping time of thiopentone anaesthesized mice and also protected
mice against the convulsive and lethal effects of pentylenetetrazole. Moreover, the ulcerogenic activity of those compounds
showing a pronounced antiinflammatory effect was also studied.
Received August 20, 2001. Accepted (revised) November 19, 2001 |
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| Keywords: | , ,Sodium saccharin, Benzenesulfonamide derivatives, Pyrazoles, Analgesic, Antiinflammatory, |
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