Literature DB >> 2874816

Crystallographic and conformational studies on histamine H1-receptor antagonists. IV. On the stereochemical vector of antihistaminic activity.

P A Borea, V Bertolasi, G Gilli.   

Abstract

The geometries of 14 histamine H1-receptor antagonists have been compared with the aim of finding out a common stereochemical vector of antihistaminic activity. The results obtained from X-ray crystallographic data have been compared with those obtained by minimizing the conformational energy of the molecules according to a simplified model of force field. Both approaches agree in indicating unique stereochemical requirements for optimum H1-antihistaminic activity.

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Year:  1986        PMID： 2874816

Source DB:  PubMed          Journal:  Arzneimittelforschung        ISSN： 0004-4172


  3 in total

1.  Computer-assisted comparison of the structural and electronic dispositions of ebastine and terfenadine.

Authors:  V Segarra; M López; H Ryder; J M Palacios; D J Roberts
Journal:  Drug Saf       Date:  1999       Impact factor: 5.606

2.  The histamine H1-receptor antagonist binding site. Part I: Active conformation of cyproheptadine.

Authors:  M J van Drooge; G M Donné-op den Kelder; H Timmerman
Journal:  J Comput Aided Mol Des       Date:  1991-08       Impact factor: 3.686

3.  Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors.

Authors:  Santosh S Kulkarni; Theresa A Kopajtic; Jonathan L Katz; Amy Hauck Newman
Journal:  Bioorg Med Chem       Date:  2006-02-03       Impact factor: 3.641
  3 in total

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