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一组N-(2-羧基苯基)苯氧基乙酰胺类新型前列腺素合成酶抑制剂的设计及其抗炎活性。

Design of a new prostaglandin synthetase inhibitors in a group of N-(2-carboxyphenyl)phenoxyacetamides and their antiinflammatory activity.

作者信息

Gryglewski R J, Ryznerski Z, Gorczyca M, Krupińska J

出版信息

Adv Prostaglandin Thromboxane Res. 1976;1:117-20.

PMID:826137
Abstract

We propose to use in vitro tests for the design of antiinflammatory drugs. These tests are inhibition of prostaglandin synthetase and binding to albumin. The antienzymic potency of a compound is a good indicator of its local antiinflammatory activity. The difference between the antienzymic and the albumin ligand potencies of a compound roughly correlates with its systemic antiinflammatory activity. We found it rewarding to use de novo models for studying structure-activity relationship within our series of prostaglandin synthetase inhibitors. It is supposed that the general chemical character of prostaglandin synthetase inhibitors inclines to a wide application of the additive mathematical model of Free and Wilson for the design of antiinflammatory drugs.

摘要

我们建议使用体外试验来设计抗炎药物。这些试验包括抑制前列腺素合成酶和与白蛋白结合。化合物的抗酶活性是其局部抗炎活性的良好指标。化合物的抗酶活性和白蛋白配体活性之间的差异大致与其全身抗炎活性相关。我们发现使用从头模型来研究我们系列前列腺素合成酶抑制剂的构效关系很有意义。据推测,前列腺素合成酶抑制剂的一般化学特性倾向于广泛应用Free和Wilson的加和数学模型来设计抗炎药物。

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