Zingel, V. and Elz, Sigurd and Schunack, W. (1993) Histamine analogues, XXXV: 2-substituted histamine derivatives containing classical moieties of H2-antagonists--a novel class of H1-agonists. Archiv der Pharmazie 326 (3), pp. 143-151.
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A new type of H1-agonists resulted from the combination of the essential histamine structure with parts of H2-antagonists. 2,4-Disubstituted imidazole derivatives were synthesized by reaction of imidic acid methyl esters with 1,3-dihydroxypropanone, 1,4-dihydroxybutanone or 2-oxo-4-phthalimido-1-butylacetate in liquid NH3. The imidazole intermediates were converted into histamine analogues by simple deprotection, Gabriel synthesis followed by deprotection, or by side-chain elongation via the nitriles and final hydrogenation. The new compounds were screened for H1-activity on the isolated guinea-pig ileum and for H2-antagonistic activity on the isolated guinea-pig right atrium. The substances are comparably weak H1-agonists and moderate H2-blockers.
|Additional information (public):||Zingel, V Elz, S Schunack, W In Vitro Germany Archiv der Pharmazie Arch Pharm (Weinheim). 1993 Mar;326(3):143-51.|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)|
|Keywords:||Animals Guinea Pigs Heart Atria/drug effects Histamine/*analogs & derivatives/chemical synthesis/pharmacology Histamine Agonists/*chemical synthesis/pharmacology Histamine H2 Antagonists/*chemical synthesis/pharmacology Muscle, Smooth/drug effects Structure-Activity Relationship|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||No|
|Owner:||Prof. Dr. Sigurd Elz|
|Deposited On:||19 Oct 2010 12:24|
|Last Modified:||19 Oct 2010 12:24|