Synthesis and histamine H3 receptor activity of 4-(n-alkyl)-1H-imidazoles and 4-(ω-phenylalkyl)-1H-imidazoles

Bioorganic and Medicinal Chemistry

Volumn 7, Issue 12, 1999, Pages 3003-3009

  De Esch, Iwan J P ^a   Gaffar, Aziz ^a   Menge, Wiro M P B ^a   Timmerman, Henk ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Antagonists; Neurologically active compounds; Neurotransmitters and receptors

Indexed keywords

4 (OMEGA PHENYLPENTYL) 1H IMIDAZOLE; 4 (PROPYL) 1H IMIDAZOLE; HISTAMINE H3 RECEPTOR; IMIDAZOLE; IMIDAZOLE DERIVATIVE; UNCLASSIFIED DRUG; ANTIHISTAMINIC AGENT;

ANIMAL TISSUE; ARTICLE; BINDING SITE; CARBON NUCLEAR MAGNETIC RESONANCE; CONTROLLED STUDY; DRUG SYNTHESIS; GUINEA PIG; JEJUNUM; LIPOPHILICITY; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; RECEPTOR AFFINITY; SMOOTH MUSCLE CONTRACTILITY; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMISTRY; DRUG EFFECT; IN VITRO STUDY; METABOLISM; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; SYNTHESIS;

ANIMALS; GUINEA PIGS; HISTAMINE ANTAGONISTS; IMIDAZOLES; JEJUNUM; MAGNETIC RESONANCE SPECTROSCOPY; RECEPTORS, HISTAMINE H3; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0033233247     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0968-0896(99)00253-9     Document Type: Article

References (19)

1. Arrang J.-M., Garbarg M., Schwartz J.-C. Neuroscience. 15:1985;553.
2. Arrang J.-M., Garbarg M., Schwartz J.-C. Nature. 302:1983;832.
3. 3 Receptor; A Target for New Drugs; Leurs, R.; Timmerman, H., Eds.; Elsevier Science B.V.: Amsterdam, 1998; p 13.
4. Arrang J.-M., Garbarg M., Lancelot J.-C., Lecomte J.-M., Pollard H., Robba M., Schunack W., Schwartz J.-C. Nature. 327:1987;117.
5. Leurs R., Blandina P., Tedford C., Timmerman H. TiPS. 19:1998;177.
6. Garbarg M., Trung Tuong M.D., Gros C., Schwartz J.-C. Eur. J. Pharmacol. 164:1989;1.
7. Leurs R., Vollinga R.C.H.T. Prog. Drug Res. 45:1995;107.
8. 3 Receptor; A Target for New Drugs; Leurs, R.; Timmerman, H., Eds.; Elsevier Science B.V.: Amsterdam, 1998; pp 223-241.
9. Oliveira L., Paiva A.C.M., Vriend G. J. Comp. -Aided Mol. Design. 7:1993;649.
10. Krause M., Ligneau X., Stark H., Garbarg M., Schwartz J.-C., Schunack W. J. Med. Chem. 41:1998;4171.
11. Ali S.M., Tedford C.E., Gregory R., Handley M.K., Yates S.L., Hirth W.W., Phillips J.G. J. Med. Chem. 5:1999;903.
12. Vollinga R.C., Menge W.M.P.B., Leurs R., Timmerman H. J. Med. Chem. 38:1995;266.
13. 3 antagonists. 11th Noordwijkerhout-Camerino Symposium, Trends in drug research, 11-15 May 1997, p 27.
14. Hüls A., Purand K., Stark H., Reidemeister S., Ligneau X., Arrang J.-M., Schwartz J.-C., Schunack W. Arch. Pharm. Med. Chem. 329:1996;379.
15. Clitherow J.W., Beswick P., Irving W.J., Scopes D.I.C., Barnes J.C., Clapham J., Brown J.D., Evans D.J., Hayes A.G. Bioorg. Med. Chem. Lett. 6:1996;833.
16. Ten Have R., Huisman M., Meetsma A., Van Lusen A.M. Tetrahedron. 53:1997;11355.
17. Horne D.A., Yakushijin K., Buchi G. Heterocycles. 39:1994;139.
18. Vollinga R.C., Zuiderveld O.P., Scheerens H., Bast A., Timmerman H. Meth. Find. Exp. Clin. Pharmacol. 14:1992;747.
19. Stark H., Ligneau X., Arrang J.-M., Schwartz J.-C., Schunack W. Bioorg. Med. Chem. Lett. 8:1998;2011.