Details

Autor(en) / Beteiligte

• 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

Titel

Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: Side chain exploration

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (7), p.1864-1868

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2006

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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 exhibited potent GHS-R antagonism and good selectivity (∼1000-fold) against dihydrofolate reductase. 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.