173459-81-9Relevant academic research and scientific papers
Synthesis and biological activity of 5-heteroaryl benzodiazepines: Analogues of YM022
Semple,Ryder,Kendrick,Szelke,Ohta,Satoh,Nishida,Akuzawa,Miyata
, p. 55 - 58 (2007/10/03)
A novel series of analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared which incorporate 5- and 6-membered heteroaromatic rings in the benzodiazepine 5-position. The 5-(2-pyridyl) derivatives in particular retained good in vitro and in vivo potency and one such compound 9i was shown to inhibit acid secretion after oral dosing in dogs. Improved bioavailability for 9i over the 5-phenyl analogue, 9h was demonstrated in rats.
Development of 1,4-Benzodiazepine Cholecystokinin Type B Antagonists
Bock, Mark G.,DiPardo, Robert M.,Evans, Ben E.,Rittle, Kenneth E.,Whitter, Willie L.,et al.
, p. 4276 - 4292 (2007/10/02)
A series of 3-(arylureido)-5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin (CCK), are described.Derived by reasoned modification of the CCK-A selective 3-carboxamido-1,4-benzodiazepine, MK-329, this paper chronicles the development of potent, orally effective compounds in which selectivity for the CCK-B recebtor subtype was achieved.The principal lead structure that emerged from these studied is L-365,260, a compound which has been submitted for clinical evaluation.Details of the ability to modulate the receptor interactions of these benzodiazepines by appropriate structure modifications are discussed which imply the possibility of further refining the CCK-B receptor affinity and selectivity of this class of compounds.
