抗过敏剂。1. 1,6 - 二氢 - 6 - 氧代 - 2 - 苯基嘧啶 - 5 - 羧酸及其酯类。
Antiallergy agents. 1. 1,6-Dihydro-6-oxo-2-phenylpyrimidine-5-carboxylic acids and esters.
作者信息
Juby P F, Hudyma T W, Brown M, Essery J M, Partyka R A
出版信息
J Med Chem. 1979 Mar;22(3):263-9. doi: 10.1021/jm00189a009.
The synthesis of some 1,6-dihydro-6-oxo-2-phenylpyrimidine-5-carboxylic acids and esters with potent oral and intravenous antiallergic activity against passive cutaneous anaphylaxis in the rat is described. Requirements for high activity include a free NH group in the pyrimidinone nucleus and a small to medium size ortho alkoxy or alkenyloxy group on the phenyl ring. It is suggested that in the case of the highly active compounds hydrogen bonding occurs between a nitrogen of the pyrimidine ring and the ethereal oxygen. The nature of this bonding and its possible contribution to an optimum configuration for the molecules is discussed.
本文描述了一些1,6 - 二氢 - 6 - 氧代 - 2 - 苯基嘧啶 - 5 - 羧酸及其酯的合成，这些化合物对大鼠被动皮肤过敏反应具有强效的口服和静脉抗过敏活性。高活性的要求包括嘧啶酮核中有一个游离的NH基团以及苯环上有一个中小尺寸的邻位烷氧基或烯氧基。有人提出，对于高活性化合物，嘧啶环的一个氮原子与醚氧之间会形成氢键。讨论了这种键合的性质及其对分子最佳构型可能的贡献。
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