91973-34-1Relevant academic research and scientific papers
Preparation of 3,4-Substituted-5-Aminopyrazoles and 4-Substituted-2-Aminothiazoles
Havel, Stepan,Khirsariya, Prashant,Akavaram, Naresh,Paruch, Kamil,Carbain, Benoit
, p. 15380 - 15405 (2019/01/04)
3,4-Substituted-5-aminopyrazoles and 4-substituted-2-aminothiazoles are frequently used intermediates in medicinal chemistry and drug discovery projects. We report an expedient flexible synthesis of 3,4-substituted-5-aminopyrazoles (35 examples), based on palladium-mediated α-arylation of β-ketonitriles with aryl bromides. A library of 4-substituted-2-aminothiazoles (21 examples) was assembled by a sequence employing Suzuki coupling of newly prepared, properly protected pinacol ester and MIDA ester of 4-boronic acid-2-aminothiazole with (hetero)aryl halides.
2,4-Diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists
Serby, Michael D.,Zhao, Hongyu,Szczepankiewicz, Bruce G.,Kosogof, Christi,Xin, Zhili,Liu, Bo,Liu, Mei,Nelson, Lissa T. J.,Kaszubska, Wiweka,Falls, H. Douglas,Schaefer, Verlyn,Bush, Eugene N.,Shapiro, Robin,Droz, Brian A.,Knourek-Segel, Victoria E.,Fey, Thomas A.,Brune, Michael E.,Beno, David W. A.,Turner, Theresa M.,Collins, Christine A.,Jacobson, Peer B.,Sham, Hing L.,Liu, Gang
, p. 2568 - 2578 (2007/10/03)
Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been shown to cause hunger and increase food intake in rodents. Inhibition of ghrelin actions with ghrelin antibody, peptidyl GHS-R antagonists, and antisense oligonucleosides resulted in weight loss and food intake decrease in rodents. Here we report the effects of GHS-R antagonists, some of which were potent, selective, and orally bioavailable. A structure-activity relationship study led to the discovery of 8a, which was effective in decreasing food intake and body weight in several acute rat studies.
