885040-87-9Relevant 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.
