Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.

@article{Elz2000HistaprodifensSP,
  title={Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.},
  author={Sigurd Elz and Kai Kramer and Heinz H. Pertz and Heiner Detert and Antonius M ter Laak and Ronald K{\"u}hne and Walter Schunack},
  journal={Journal of medicinal chemistry},
  year={2000},
  volume={43 6},
  pages={1071-84}
}
A new class of histamine analogues characterized by a 3, 3-diphenylpropyl substituent at the 2-position of the imidazole nucleus has been prepared outgoing from 4,4-diphenylbutyronitrile (4b) via cyclization of the corresponding methyl imidate 5b with 2-oxo-4-phthalimido-1-butyl acetate or 2-oxo-1,4-butandiol in liquid ammonia, followed by standard reactions. The title compounds displayed partial agonism on contractile H(1) receptors of the guinea-pig ileum and endothelium-denuded aorta… CONTINUE READING

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