6533b871fe1ef96bd12d104c

RESEARCH PRODUCT

H2-antihistaminics. 20. Structure-activity relationships in H2-receptor antagonists containing a 4-pyrimidone moiety.

J. P. SpenglerWalter SchunackK. Wegner

subject

PharmacologyStereochemistryImmunologyPharmacology toxicologyGuinea PigsHeartPyrimidinonesToxicologyLipidschemistry.chemical_compoundStructure-Activity RelationshipDrug activitychemistryHistamine H2 receptorHistamine H2 AntagonistsSolubilityLipophilicityMoietyAnimalsPharmacology (medical)Pyrimidone

description

In a series of 5,6-substituted 4- pyrimidones 1 a-v the H2-antihistaminic activity was determined (guinea-pig atrium) and lipophilicity data are given in form of Rmo -values. The influence of different substituents at position 5 or 6 of a pyrimidone moiety has been studied. Quantitative structure-activity analyses showed the importance of lipophilicity for drug activity. Additionally other physicochemical substituent-properties may play a major role.

yearjournalcountryeditionlanguage
1984-05-01Agents and actions
10.1007/bf01973873https://pubmed.ncbi.nlm.nih.gov/6145340