28991-24-4Relevant academic research and scientific papers
Recyclable Pd/CuFe2O4 nanowires: A highly active catalyst for C-C couplings and synthesis of benzofuran derivatives
Lakshminarayana, Bhairi,Chakraborty, Jhonti,Satyanarayana,Subrahmanyam, Ch.
, p. 21030 - 21039 (2018)
Pd/CuFe2O4 nanowire-catalyzed cross coupling transformations are described. Notably, these reactions showed excellent functional group tolerance. Further, the protocol is applied to a one-pot synthesis of benzofurans via a Sonogashira coupling and intramolecular etherification sequence. The catalyst was reused and found to maintain its activity and stability.
Novel inhibitors of chymase
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Page/Page column 28, (2008/06/13)
The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates and derivatives thereof, and met
Optimization of 3-(1H-Indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists
Henke, Brad R.,Aquino, Christopher J.,Birkemo, Larry S.,Croom, Dallas K.,Dougherty Jr., Robert W.,Ervin, Gregory N.,Grizzle, Mary K.,Hirst, Gavin C.,James, Michael K.,Johnson, Michael F.,Queen, Kennedy L.,Sherrill, Ronald G.,Sugg, Elizabeth E.,Suh, Edward M.,Szewczyk, Jerzy W.,Unwalla, Rayomand J.,Yingling, Jeff,Willson, Timothy M.
, p. 2706 - 2725 (2007/10/03)
We previously described a series of 3-(1H-indazol-3-ylmethyl)-1,5- benzodiazepine CCK-A agonists exemplified by compound 1 (GW 5823), which is the first reported binding selective CCK-A full agonist demonstrating oral efficacy in a rat feeding model. In this report we describe analogs of compound 1 designed to explore changes to the CS and N1 pharmacophores and their effect on agonist activity and receptor selectivity. Agonist efficacy in this series was affected by stereoelectronic factors within the C3 moiety. Binding affinity for the CCK-A vs CCK-B receptor showed little dependence on the structure of the C3 moiety but was affected by the nature of the second substituent at CS. Structure-activity relationships at the N1- anilidoacetamide 'trigger' moiety within the C3 indazole series were also investigated. Both agonist efficacy and binding affinity within this series were modulated by variation of substituents on the Nl-anilidoacetamide moiety. Evaluation of several analogs in an in vivo mouse gallbladder emptying assay revealed compound 1 to be the most potent and efficacious of all the analogs tested. The pharmacokinetic and pharmacodynamic profile of 1 in rats is also discussed.
