Bioorganic and Medicinal Chemistry Letters p. 1864 - 1868 (2006)
Update date:2022-07-29
Topics:
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
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.
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