Many derivatives of heterocyclic compounds containing a sulfonamide thiazole moiety were synthesized through the reaction of 2-(cyano or chloro)-N-(4-(N-thiazol-2-ylsulfamoyl)phenyl)acetamide with isocyanate followed by halogenated compounds, arylidene, 2-hydroxy benzaldehydes, active methylene compounds, and heterocyclic amines. The anticonvulsant activity for 15 of the synthesized compounds was evaluated and 6 compounds showed protection against picrotoxin-induced convulsion. 4-(6-Amino-3,5-dicyano-4-(4-methoxyphenyl)-2-oxopyridin-1(2H)-yl)-N-(thiazol-2-yl)benzenesulfonamide (11b) exhibited significant anticonvulsive effects, abolished the tonic extensor phase and offered 100% protection.
Searching for new anti-inflammatory and analgesic agents, we have prepared a series of novel pyrazoles containing benzofuran and trifluoromethyl moieties. The pyrazole derivatives have been synthesized via two routes starting from 5-(3-(trifluoromethyl)phenyl azo) salicylaldehyde. The first route involved the synthesis of 2-acetylbenzofuran and then treatment with aldehydes to afford the corresponding chalcones. The cyclization of the latter chalcones with hydrazine hydrate led to the formation of new pyrazoline derivatives. The second route involved the synthesis of benzofuran-2-carbohydrazide and then treatment with formylpyrazoles, chalcones and ketene dithioacetal derivatives to afford the corresponding pyrazole derivatives. Some of the synthesized compounds exhibited anti-inflammatory and analgesic activities.
Synthesis of Pyrazoles Containing Benzofuran and Trifluoromethyl Moieties as Possible Antiinflammatory and Analgesic Agents. -Some of the synthesized compounds exhibit good antiinflammatory and/or significant analgesic activities. -(FARAG, A. A.; EL SHEHRY, M. F.; ABBAS*, S. Y.; ABD-ALRAHMAN, S. N.; ATREES, A. A.; AL-BASHEER, H. Z.; AMMAR, Y. A.; Z. Naturforsch., B: Chem. Sci. 70 (2015) 7, 519-526, http://dx.
A variety of azole, pyridine and chromene derivatives incorporating a sulfonamide moiety are synthesized and evaluated for their anticonvulsant activity.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.