Title of article :
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
Author/Authors :
Graham A. Showell، نويسنده , , Sylvie Bourrain، نويسنده , , Stephen R. Fletcher، نويسنده , , Joseph G. Neduvelil، نويسنده , , Alan E. Fletcher، نويسنده , , Stephen B. Freedman، نويسنده , , Smita Patel، نويسنده , , Alison J. Smith، نويسنده , , George R. Marshall، نويسنده , , Michael I. Graham، نويسنده , , Bindi Sohal، نويسنده , , Victor G. Matassa، نويسنده ,
Abstract :
A novel series of potent, water-soluble benzodiazepine based CCKB/gastrin antagonists has been prepared which incorporate an N-methylpiperazine group at the C5 position of the benzodiazepine ring system. The N1-n-propyl analogue (7b) is a high affinity, selective and potent receptor antagonist in vitro, with good bioavailability and excellent oral absorption providing high plasma levels in vivo.
