166388-36-9Relevant academic research and scientific papers
Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists
Kawanishi, Yasuyuki,Ishihara, Shoichi,Tsushima, Tadahiko,Seno, Kaoru,Miyagoshi, Masanori,Hagishita, Sanji,Ishikawa, Michio,Shima, Noriko,Shimamura, Mayumi,Ishihara, Yasunobu
, p. 1421 - 1426 (2007/10/03)
The joint type of hybrid molecules composed of two pharmacophore moieties taken from histamine H2 and gastrin receptor antagonists have been designed and synthesized to exhibit dual histamine H2 and gastrin receptor antagonistic activities. Here we report the importance of spacers as well as binding sites of both pharmacophores for the dual activity.
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.
