861102-81-0Relevant academic research and scientific papers
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: Side chain exploration
Liu, Bo,Liu, Mei,Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Kosogof, Christi,Nelson, Lissa T.J.,Szczepankiewicz, Bruce G.,Kaszubska, Wiweka,Schaefer, Verlyn G.,Falls, H. Douglas,Lin, Chun Wel,Collins, Christine A.,Sham, Hing L.,Liu, Gang
, p. 1864 - 1868 (2007/10/03)
The synthesis and structure-activity relationships of the 4- and 6-substituents of 2,4-diaminopyrimidine-based growth hormone secretagogue receptor (GHS-R) antagonists are described. Diaminopyrimidines with 6-norbornenyl (4n) and 6-tetrahydrofuranyl (4p) substitutents were found to exhibit potent GHS-R antagonism and good selectivity (～1000-fold) against dihydrofolate reductase.
Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (GHS-R) antagonists
-
Page/Page column 44, (2010/02/13)
The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.
