Literature DB >> 6145340

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

J P Spengler, K Wegner, W Schunack.   

Abstract

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.

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Year:  1984        PMID： 6145340     DOI： 10.1007/bf01973873

Source DB:  PubMed          Journal:  Agents Actions        ISSN： 0065-4299


  6 in total

1.  Rm values of steroids as an expression of their lipophilic character in structure-activity studies.

Authors:  G L Biagi; A M Barbaro; O Gandolfi; M C Guerra; G Cantelli-Forti
Journal:  J Med Chem       Date:  1975-09       Impact factor: 7.446

2.  Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters.

Authors:  J M VAN ROSSUM
Journal:  Arch Int Pharmacodyn Ther       Date:  1963

Review 3.  Evidence for and against heterogeneity in the histamine H2-receptor population.

Authors:  G Bertaccini; G Coruzzi
Journal:  Pharmacology       Date:  1981       Impact factor: 2.547

4.  Quantitative structure--activity relationships. 7. The bilinear model, a new model for nonlinear dependence of biological activity on hydrophobic character.

Authors:  H Kubinyi
Journal:  J Med Chem       Date:  1977-05       Impact factor: 7.446

5.  [Synthesis and H2-antihistaminic activity of ring methylated metiamide analogues. 4th communication: H2-antihistaminic agents (author's transl)].

Authors:  W Schunack; H Engler; E Fritschi
Journal:  Arzneimittelforschung       Date:  1979

6.  [H2-Antihistaminics, 11: Cyclic guanidines with H2-antihistaminic activity].

Authors:  J P Spengler; W Schunack
Journal:  Arch Pharm (Weinheim)       Date:  1983-01       Impact factor: 3.751
  6 in total

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