Zingel, V. and Elz, Sigurd and Schunack, W. (1992) Histamine analogues. 36th communication. Basically substituted histamine derivatives with H1-agonistic activity. Pharmazie 47 (10), pp. 746-751.
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Piperidinoalkyl-, morpholinoalkyl- or [(pyrid-2-yl)methylthio]alkyl-substituents were introduced into position 2 of the essential histamine structure. These 2-substituted histamine derivatives were prepared via reaction of imidate hydrochlorides in liquid ammonia under pressure with 1,3-dihydroxypropanone followed by a stepwise build-up of the side chain in position 4 of the imidazole nucleus (route I) or by cyclization with 2-oxo-4-phthalimido-1-butyl acetate (route II) followed by deprotection of the primary amine function. The novel compounds were screened for H1-activity on the isolated guinea-pig ileum and for H2-activity on the isolated guinea-pig right atrium. While 10a, c-e proved to be weak partial H1-agonists, 10b, f were very weak H1-antagonists.
|Additional information (public):||Zingel, V Elz, S Schunack, W In Vitro Research Support, Non-U.S. Gov't Germany Die Pharmazie Pharmazie. 1992 Oct;47(10):746-51.|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)|
|Keywords:||Animals Guinea Pigs Heart Atria/drug effects Histamine/*analogs & derivatives/pharmacology Histamine Agonists/*chemical synthesis/pharmacology Ileum/drug effects Muscle Contraction/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 14:29|
|Last Modified:||19 Oct 2010 14:29|
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