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4-芳基-1-异丙基-2(1H)-喹唑啉酮系列五个成员的抗炎及其他药效学特性

Anti-inflammatory and other pharmacodynamic properties of five members of the 4-aryl-1-isopropyl-2(1H)-quinazolinone series.

作者信息

Perrine J W, Houlihan W J, Takesue E I

出版信息

Arzneimittelforschung. 1984;34(8):879-85.

PMID:6333879
Abstract

A series of five 4-aryl-1-isopropyl-2(1H)-quinazolinone analogs were examined for their relative activities regarding analgesia, suppression of inflammation and pyresis, and associated phenomena. Two of these, proquazone (SaH 43-715, Biarsan, Biarison) and fluproquazone (SaH 46-790), are clinically effective anti-inflammatory and analgesic agents. Acetylsalicylic acid (ASA) and phenylbutazone were included for reference as first and second generation nonsteroidal anti-inflammatory drugs (NSAID), respectively. In general, substitutions in these five quinazolinone analogs produced noticeable changes in potency in several activities but changes of lesser degrees in others. Compared to ASA and phenylbutazone the quinazolinones exhibited better analgesic and related activities.

摘要

研究了一系列五个4-芳基-1-异丙基-2(1H)-喹唑啉酮类似物在镇痛、抗炎、解热及相关现象方面的相对活性。其中两种,丙酰苯吡唑酮(SaH 43-715,必来松,比亚里松)和氟丙酰苯吡唑酮(SaH 46-790)是临床上有效的抗炎和镇痛药。分别将阿司匹林(ASA)和保泰松作为第一代和第二代非甾体抗炎药(NSAID)纳入作为参考。一般来说,这五个喹唑啉酮类似物中的取代基在几种活性中产生了显著的效力变化,但在其他活性中变化较小。与ASA和保泰松相比,喹唑啉酮表现出更好的镇痛及相关活性。

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