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2-酰基-5(3)-羟基四氢-1H-吡唑衍生物的抗炎活性

Anti-inflammatory activity of 2-acyl-5(3)-hydroxytetrahydro-1H-pyrazole derivatives.

作者信息

Zelenin K N, Bezhan I P, Pastushenkov L V, Gromova E G, Lesiovskaja E E, Chakchir B A, Melnikova L F

机构信息

Department of Chemistry of Military Medical Academy, St. Petersburg, Russia.

出版信息

Arzneimittelforschung. 1999 Oct;49(10):843-8. doi: 10.1055/s-0031-1300512.

Abstract

The anti-inflammatory effects of five pyrazolidine derivatives on white mice and laboratory rats were studied using models of thermal aseptic inflammation and inflammation induced by injection of carragenin and histamine, as well as models of "cotton-ball granuloma" and epinephrine (adrenaline)-induced pulmonary edema. These effects were compared with those of the most commonly used non-steroid anti-inflammatory drugs, such as phenylbutazone (CAS 50-33-9) and diclofenac (CAS 15307-79-6). It was found that the pyrazolidine compounds studied induced a pronounced anti-inflammatory effect by inhibiting both the proliferative and exudative phases of inflammation. At the same time, as compared to natural non-steroid anti-inflammatory drugs, these compounds had a lower toxicity and induced neither gastric ulcers nor suppression of hemopoiesis.

摘要

利用热无菌性炎症模型、注射角叉菜胶和组胺诱导的炎症模型,以及“棉球肉芽肿”模型和肾上腺素诱导的肺水肿模型,研究了五种吡唑烷衍生物对小白鼠和实验大鼠的抗炎作用。将这些作用与最常用的非甾体抗炎药,如保泰松(CAS 50-33-9)和双氯芬酸(CAS 15307-79-6)的作用进行了比较。结果发现,所研究的吡唑烷化合物通过抑制炎症的增殖期和渗出期,产生了显著的抗炎作用。同时,与天然非甾体抗炎药相比,这些化合物毒性较低,既不会引起胃溃疡,也不会抑制造血。

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Nonsteroidal anti-inflammatory activity of 1,2,4-triazolyl-heterocarboxylic derivatives.
Arzneimittelforschung. 1999 Jun;49(6):514-8. doi: 10.1055/s-0031-1300453.

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