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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands.

Para-substituted aromatic ethers with benzophenone or related structural elements and a 3-(1H-imidazol-4-yl)propyloxy moiety were prepared by Mitsunobu-type ether synthesis or SNAr reaction. Most of the title compounds possess high antagonist potency in histamine H3-receptor assays in vitro as well as in vivo in mouse CNS following oral administration. After defining 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl phenyl methanone as a new lead, structure-activity relationships were investigated for this new class of compounds. Substitution of the meta'-position of the benzophenone moiety with halogen atoms (e.g., iodine, fluorine) led to compounds with high antagonist potency in vitro as well as in vivo (Ki = 9.3 and 4.3 nM, ED50 = 0.7 and 0.47 mg/kg p.o., 18 and 12, respectively). A receptor profile of several functional in vitro assays for several biogenic amine receptors for the meta'-iodinated derivative demonstrated high selectivity toward the histamine H3 receptor.[1]

References

  1. Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands. Sasse, A., Ligneau, X., Sadek, B., Elz, S., Pertz, H.H., Ganellin, C.R., Arrang, J.M., Schwartz, J.C., Schunack, W., Stark, H. Arch. Pharm. (Weinheim) (2001) [Pubmed]
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