Title of article
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: Side chain exploration
Author/Authors
Bo Liu، نويسنده , , Mei Liu، نويسنده , , Zhili Xin، نويسنده , , Baolin Wu&Hongyu Zhao، نويسنده , , Michael D. Serby، نويسنده , , Christi Kosogof، نويسنده , , Lissa T.J. Nelson، نويسنده , , Bruce G. Szczepankiewicz، نويسنده , , Wiweka Kaszubska، نويسنده , , Verlyn G. Schaefer، نويسنده , , H. Douglas Falls، نويسنده , , Chun Wel Lin، نويسنده , , Christine A. Collins، نويسنده , , Hing L. Sham، نويسنده , , Gang Liu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
1864
To page
1868
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.
Keywords
DHFR selectivity , GHS-R antagonist , ghrelin , Diaminopyrimidine
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796680
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