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Synthesis and biological evaluation of some novel sulfamoylphenyl-pyridazinone as anti-inflammatory agents (Part-II*)

机译:某些新型氨磺酰基苯基-哒嗪酮类抗炎药的合成和生物学评价(第二部分*)

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Seven novel 6-aryl-2-(p-sulfamoylphenyl)-4,5-dihydropyridazin-3(2H)-ones (2a-g) were synthesized by the condensation of appropriate aroylpropionic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Structure of all compounds have been elucidated by elemental analysis, IR, 1H NMR, 13C NMR, DEPT and MS spectrscopy. These compounds were tested for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Compound 2b exhibited anti-inflammatory activity comparable to that of celecoxib (at 5?h). Two other compounds 2d and 2g showed promising anti-inflammatory activity (edema reduction more than 80% at 5?h). These compounds (2b, 2d and 2g) did not produce any ulceration in gastric region.
机译:通过将合适的芳酰基丙酸和4-肼基苯磺酰胺盐酸盐在乙醇中缩合,合成了七个新颖的6-芳基-2-(对氨基磺酰基苯基)-4,5-二氢哒嗪-3(2H)-一(2a-g)。通过元素分析,IR, 1 1 H NMR, 13 C NMR,DEPT和MS光谱对所有化合物的结构进行了阐明。在角叉菜胶诱导的大鼠爪水肿模型中测试了这些化合物的抗炎活性。化合物2b的抗炎活性与塞来昔布相当(在5?h时)。另外两种化合物2d和2g显示出有希望的抗炎活性(5?h时水肿减少超过80%)。这些化合物(2b,2d和2g)在胃区域未产生任何溃疡。

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