Synthesis and anthelmintic activity of a series of of pyrazino[2,1-a][2]benzazepine derivatives

A series of 1,2,3,4,6,7,8,12b-octahydropyrazino[2,1-alpha][2] benzazepine derivatives was prepared and the cestocidal activity of the compounds evaluated in an in vitro Taenia crassiceps screen. Many of these derivatives proved to be highly active, and 2-(cyclohexylcarbonyl)-4-oxo-1,2,3,4,6,7,8,12b-...

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Veröffentlicht in:	Journal of medicinal chemistry 1989-09, Vol.32 (9), p.2058-2062
Hauptverfasser:	Brewer, Malcolm D, Burgess, Malcolm N, Dorgan, Roderick J. J, Elliott, Richard L, Mamalis, Patrick, Manger, Brian R, Webster, Richard A. B
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals anthelmintic agents Anticestodal Agents - chemical synthesis Anticestodal Agents - pharmacology Anticestodal Agents - therapeutic use Benzazepines - chemical synthesis Benzazepines - pharmacology Benzazepines - therapeutic use Chemical Phenomena Chemistry Dogs Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Isomerism Organic chemistry Preparations and properties Structure-Activity Relationship Taenia - drug effects Taeniasis - drug therapy
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Zusammenfassung:	A series of 1,2,3,4,6,7,8,12b-octahydropyrazino[2,1-alpha][2] benzazepine derivatives was prepared and the cestocidal activity of the compounds evaluated in an in vitro Taenia crassiceps screen. Many of these derivatives proved to be highly active, and 2-(cyclohexylcarbonyl)-4-oxo-1,2,3,4,6,7,8,12b- octahydropyrazino[2,1-alpha][2]benzazepine, epsiprantel (BAN) (22), was selected for further development. The structure-activity relationships are discussed.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00129a007