147283-46-3Relevant articles and documents
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation
Debenham, John S.,Madsen-Duggan, Christina B.,Wang, Junying,Tong, Xinchun,Lao, Julie,Fong, Tung M.,Schaeffer, Marie-Therese,Xiao, Jing Chen,Huang, Cathy C.R.-R.,Shen, Chun-Pyn,Sloan Stribling,Shearman, Lauren P.,Strack, Alison M.,Euan MacIntyre,Hale, Jeffrey J.,Walsh, Thomas F.
scheme or table, p. 2591 - 2594 (2009/12/25)
The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indicate
Heterocyclic amides
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, (2008/06/13)
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Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, synthesis, and in vitro activity of a series of 3-amino-6-arylopyridin-2-one trifluoromethyl ketones
Damewood Jr.,Edwards,Feeney,Gomes,Steelman,Tuthill,Williams,Warner,Woolson,Wolanin,Veale
, p. 3303 - 3312 (2007/10/02)
A series of potent nonpeptidic inhibitors of the enzyme human leukocyte elastase (HLE) is reported. These inhibitors contain a 3-amino-2-pyridone ring as a central template in which the pyridone carbonyl and 3-position NH group are thought to form important hydrogen bonding interactions with the Val-216 residue of HLE. Substitution of the 6-position of the pyridone ring by various alkyl and aryl groups was found to afford increases in the in vitro potency of these inhibitors. A 6-position phenyl group, compound 10f, was found to result in a large increase in binding affinity, which was not obtained when the phenyl group was placed in either the 4- or 5-position of the molecule. Compound 10f was found to have good selectivity for HLE over other proteolytic enzymes, with the exception of bovine pancreatic chymotrypsin (BPC). Substitution of the 6-phenyl group in these molecules was found to decrease binding affinity for BPC without adversely affecting affinity for HLE.