C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists

Abstract A novel series of potent, water-soluble benzodiazepine based CCK B /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 .