Abstract
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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