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

@article{Borea1986CrystallographicAC,
  title={Crystallographic and conformational studies on histamine H1-receptor antagonists. IV. On the stereochemical vector of antihistaminic activity.},
  author={Pier Andrea Borea and Valerio Bertolasi and Gastone Gilli},
  journal={Arzneimittel-Forschung},
  year={1986},
  volume={36 6},
  pages={895-9}
}
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.