Quinazoline-2,4-dione誘導体,H-27およびH-88に関する薬理学的研究-1-抗炎症,鎮痛および下熱作用について

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From the screening tests of many compounds quinazoline-2, 4-dione derivatives were found to possess anti-inflammatory activities. About 400 compounds of these derivatives have been synthesized in order to investigate their inhibitory actions on carrageenin-induced edema and acetic acid-induced writhing. 1-(m-trifluoromethylpheny 1) -3 ethyl-quinazoline-2, 4-dione (H-27) and 1-(m-trifluoromethylphenyl)-3-(2'-hydroxy)-ethyl-quinazoline-2, 4-dione (H-88) demonstrated the most effective activities. Both compounds inhibited increased vascular permeability and the acute edema induced by various stimulations, and the activities were less than those of indomethacin, but more potent than those of phenylbutazone, flufenamic acid, benzydamine and mepirizole. The effect of test compounds on the acute edema was decreased by adrenalectomy or myelotomy, but did not disappear and slight thymolytic action was evidenced. H-27 exerted slight inhibitory effects on ultraviolet erythema, granuloma formation and adjuvant arthritis. H-88 did not inhibit subacute inflammatory reactions nor did it produce gastric ulceration. On the other hand, H-88 had analgesic and antipyretic actions and the activities were about twice as potent as those of aminopyrine and 4 times those of mefenamic acid, while H-27 showed none of those actions. Consequently, it may be considered that H-88 is a new type of non-steroid anti-inflammatory agent with potent analgesic and antipyretic activities.
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Quinazoline-2,4-dione誘導体,H-27およびH-88に関する薬理学的研究-1-抗炎症,鎮痛および下熱作用について

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