72716-93-9Relevant academic research and scientific papers
Isocytosine H2-receptor histamine antagonists II. Synthesis and evaluation of biological activity at histamine H1- and H2-receptors of 5-(heterocyclyl)methylisocytosines
Brown, Thomas H.,Blakemore, Robert C.,Blurton, Peter,Durant, Graham J.,Ganellin, C. Robin,et al.
, p. 65 - 72 (2007/10/02)
A series of 2--4-pyrimidones was synthesized based on oxmetidine 2, in which the methylenedioxyphenyl group of 2 was replaced by a heterocyclic ring.Good H2-receptor antagonist activity was retained over a range of basic and neutral heterocyclic substituents.Replacement of the 5-methyl-4-imidazolyl ring in selected compounds with 2-thiazolyl and, particularly, 3-bromo-2-pyridyl rings gave a series of compounds which have both H1- and H2-receptor histamine antagonist activities.Some structure-activity and structure-toxicity correlations are discussed.Compound 6d, 2--5-(6-methylpyrid-3-yl)-4-pyrimidone, has the most favourable combination of properties for H2-antagonism and has been evaluated further as an anti-secretory agent.
GUANIDINOTHIAZOLYL DERIVATIVES
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, (2008/06/13)
The compounds are guanidinothiazolyl derivatives which are histamine H. sub.2-antagonists. A specific compound of the present invention is 2-2-(2-guanidino-4-thiazolylmethylthio)ethylamino!-5-(6-methyl-3-pyridylmethy l)-4-pyrimidone.
ISOUREAS AND ISOTHIOUREAS
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, (2008/06/13)
The compounds are isoureas and isothioureas which have an O-or S-alkylpyrimidone substituent and which are histamine H 2-antagonists and antiinflammatory agents. A specific compound of this invention is 2-[5-(O-isoureido)pentylamino]-5-(6-methyl-3-pyridylmethyl)-4-pyrimidone.
Intermediates in the process for making histamine antagonists
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, (2008/06/13)
A process for making substituted 2-aminopyrimidones which are histamine H2 - antagonists which comprises reacting a 2-nitroaminopyrimidone with a heteroarylalkylamine, heteroarylalkylthioalkylamine, or heteroarylalkoxyalkylamine. One particular compound which can be made by this process is 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-[5-(1,3-benzodioxolyl)methyl]-4-pyrimidone. Also claimed are 2-nitroaminopyrimidone intermediates for use in this process. One specific intermediate is 2-nitroamino-5-[5-(1,3-benzodioxolyl)methyl]-4-pyrimidone.
Pyrimidine compounds
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, (2008/06/13)
The compounds are substituted pyrimidine compounds which are histamine H2 -antagonists. A specific compound of the present invention is 2-[2-(5-dimethylaminomethyl)-2-furylmethylthio)ethylamino]-5-(3-pyridylmethyl)-4-pyrimidone.
