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  • Title: Crystallographic and conformational studies on histamine H1-receptor antagonists. IV. On the stereochemical vector of antihistaminic activity.
    Author: Borea PA, Bertolasi V, Gilli G.
    Journal: Arzneimittelforschung; 1986 Jun; 36(6):895-9. PubMed ID: 2874816.
    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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