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C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists |
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| Authors: | Graham A. Showell Sylvie Bourrain Stephen R. Fletcher Joseph G. Neduvelil Alan E. Fletcher Stephen B. Freedman Smita Patel Alison J. Smith George R. Marshall Michael I. Graham Bindi Sohal Victor G. Matassa |
| Affiliation: | Merck, Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, United Kingdom |
| 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. |
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