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[一种新型含氮多环体系。苯并呋喃和噻吩并噻二唑嘧啶衍生物的合成与药理性质。I]

[A new nitrogen-containing polycyclic system. Synthesis and pharmacologic properties of benzofuran and thienothiadiazolepyrimidine derivatives. I].

作者信息

Russo F, Santagati M, Santagati A, Caruso A, Trombatore S, Amico Roxas M

出版信息

Farmaco Sci. 1983 Oct;38(10):762-74.

PMID:6605880
Abstract

A series of 5H-benzofuro[3,2-d]1,3,4-thiadiazolo[3,2-a]-pyrimidin-5-ones and 1,3,4-thiadiazolo[3,2-a]thieno[2,3-d]pyrimidin-5-ones were synthesized and their analgesic, antiinflammatory, antiexudative and ulcerogenic activities were evaluated. The analgesic and antiexudative activities of several derivatives proved to be less than that of indomethacin and much higher than that of mefenamic and acetylsalicylic acids. Acute toxicity and ulcerogenic effects were significantly lower than those of reference drugs.

摘要

合成了一系列5H-苯并呋喃[3,2-d]1,3,4-噻二唑并[3,2-a]嘧啶-5-酮和1,3,4-噻二唑并[3,2-a]噻吩并[2,3-d]嘧啶-5-酮,并对它们的镇痛、抗炎、抗渗出和致溃疡活性进行了评估。几种衍生物的镇痛和抗渗出活性被证明低于吲哚美辛,但远高于甲芬那酸和乙酰水杨酸。急性毒性和致溃疡作用明显低于参比药物。

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