Histamine H2-receptor agonists. Synthesis, in vitro pharmacology, and qualitative structure-activity relationships of substituted 4-and 5-(2-aminoethyl) thiazoles

JC Eriks, H Van der Goot, GJ Sterk…

Index: Eriks; Van der Goot; Sterk; Timmerman Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3239 - 3246

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Citation Number: 83

Abstract

It is well known that both histamine and dimaprit show moderate histamine Hz-receptor agonistic activities on the guinea pig right atrium. Quantum chemical calculations on these two compounds showed similarities in electron distributions and molecular electrostatic potentials (MEP's), which could be extended. to rigid analogues [2-amino-5-(2-aminoethyl) thiaoles] of the latter structure. On the base of these results a series of substituted 4-and 5- ...