Abstract
Abstract: In the present work, a series of 3-indolyldihydropyrimidine thione containing pyrazole, thiadiazole, and/or benzothiazole were prepared in the form of sulfonamide and sulfohydrazide derivatives in either conventional conditions or under microwave irradiation and evaluated as potential non-steroidal cyclooxygenase-2(COX-2) inhibitors. On subjecting the key synthon 1-[4-(1H-Indol-3-yl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl]-3,3-dimercaptopropene 1 to the reaction with phenylhydrazine; pyrazole condensed to indolyldihydropyrimidine 2 formed and used as a starting material for synthesizing pyrazoles sulfohydrazides and pyrazole sulfonamides moieties. The newly synthesized target compounds have been examined as in vitro antimicrobial agents and in vivo anti-inflammatory and analgesic according to carrageenan-induced paw edema in comparison with celecoxib as a standard drug; promising activities were obtained. All newly obtained compounds have been characterized by means of elemental and spectral analyses, e.g. FT-IR, Mass spectra, 1H NMR, and 13C NMR.
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