29639-77-8Relevant articles and documents
Design, synthesis and evaluation of MCH receptor 1 antagonists - Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414
Müller, Stephan G.,Heckel, Armin,Kley, J?rg T.,Lehmann, Thorsten,Lustenberger, Philipp,Oost, Thorsten,Roth, Gerald J.,Rudolf, Klaus,Arndt, Kirsten,Lenter, Martin,Lotz, Ralf R.H.,Maier, Gerd-Michael,Markert, Michael,Schindler, Marcus,Stenkamp, Dirk
, p. 3264 - 3269 (2015/07/08)
Abstract Despite recent approvals of anti-obesity drugs there is still a high therapeutic need for alternative options with higher efficacy in humans. As part of our MCH-R1 antagonist program for the treatment of obesity, a series of biphenylacetamide HTS
The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy)caffeine analogues
Strydom,Bergh,Petzer
, p. 513 - 518 (2013/01/15)
Previous studies have documented that substituted 8-oxycaffeines act as inhibitors of human monoamine oxidase (MAO) B. A particularly potent inhibitor among the reported compounds was 8-(2-phenoxyethoxy)caffeine with an IC 50 value of 0.383M towards MAO-B. In an attempt to improve on the inhibition potency of this compound and to discover highly potent reversible MAO-B inhibitors, in the present study, a series of 8-(2-phenoxyethoxy)caffeine analogues containing various substituents on C4 of the phenoxy ring, were synthesized and evaluated as inhibitors of human MAO-A and -B. The results show that the 8-(2-phenoxyethoxy)caffeine analogues are selective and reversible MAO-B inhibitors with the most potent homologue, 8-{2-[4-(trifluoromethyl) phenoxy]ethoxy}caffeine, exhibiting an IC50 value of 0.061μM. These highly potent inhibitors are useful leads in the design of therapies for neurodegenerative disorders such as Parkinsons disease. Georg Thieme Verlag KG Stuttgart New York.
NEW PYRIDAZINE DERIVATIVES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
-
Page/Page column 96, (2008/12/06)
The present invention relates to compounds of general formula I wherein the groups and radicals B, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.