- Synthesis and Anthelmintic Activity of a Series of Pyrazinobenzazepine Derivatives
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A series of 1,2,3,4,6,7,8,12b-octahydropyrazinobenzazepine 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-octahydropyrazinobenzazepine, epsiprantel (BAN) (22), was selected for further development.The structure-activity relationships are discussed.
- Brewer, Malcolm D.,Burgess, Malcolm N.,Dorgan, Roderick J. J.,Elliott, Richard L.,Mamalis, Patrick,et al.
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p. 2058 - 2062
(2007/10/02)
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- Benzazepines, and their use as anthelminthics
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A compound of formula (I): STR1 in which R is optionally substituted phenyl; C3-8 cycloalkyl; C5-8 cycloalkenyl; C1-8 alkyl which may be straight or branched; C2-8 alkenyl which may be straight or branched; 5- or 6- membered heterocyclyl; or optionally substituted phenyl C1-4 alkyl, each of Y and Z, which may be the same or different, is oxygen or sulphur; and X is --CH2 -- or oxygen, a process for the preparation of such compounds and their use in human and veterinary medicine.
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