Crystallographic and conformational studies on histamine H1-receptor antagonists. IV. On the stereochemical vector of antihistaminic activity.
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.
D003461:Crystallography; D006634:Histamine H1 Antagonists / Q000032:analysis* / Q000494:pharmacology; D008968:Molecular Conformation; D013237:Stereoisomerism
D006634:Histamine H1 Antagonists