Pseudosymmetry and bioisosterism in biaryl pyridyl competitive histamine H2-receptor antagonists

CA Lipinski, JL LaMattina…

Index: Lipinski, Christopher A.; LaMattina, John L.; Hohnke, Lyle A. Journal of Medicinal Chemistry, 1985 , vol. 28, # 11 p. 1628 - 1636

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Citation Number: 22

Abstract

A process of drug design has previously been described that led to the synthesis of 3-amino- 5-[2-(ethylamino)-4-pyridyl]-1, 2, 4-triazole (4), a competitive histamine H2-receptor antagonist structurally unrelated to, but more potent than, cimetidine. A QSAR study on a subset of analogues closely related to 4 showed that gastric acid antisecretory activity increased with decreasing lipophilicity. An SAR study about 4 focused on (1) pyridine ...