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Khaled R. A. Abdellatif,Mohamed A. Abdelgawad,Heba A. H. Elshemy,Shahinda S. R. Alsayed 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.11
Anovel series of 2-pyrazoline derivatives 13a–l wassynthesized via aldol condensation of 4-substituted acetophenoneswith appropriately substituted aldehydes followed by cyclizationof the formed chalcones with 4-hydrazinobenzenesulfonamidehydrochloride. The chemical structures of the targetpyrazoline derivatives were proved by means of IR, 1HNMR, 13CNMR, mass spectroscopy and elemental analyses data. All thesynthesized compounds were evaluated for their cyclooxygenaseselectivity, anti-inflammatory and ulcerogenic liability. Whilecompounds 13e, 13h and 13i showed moderate COX-2 selectivityin vitro and good anti-inflammatory activity in vivo, compound13i showed the highest anti-inflammatory activity that isvery close in potency to the reference drug (celecoxib) with bettergastric profile than celecoxib.