3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.
The synthesis of a series of 3-aryl pyrazolo[4,3-d]pyrimidines as potential corticotropin-releasing factor (CRF-1) antagonists is described. The effects of substitution on the aromatic ring, the amino group and the pyrazolo ring on CRF-1 receptor binding were investigated.
Yuan
Jun
J
Neurogen Corporation, 35Northeast Industrial Road, Branford, CT 06405, USA.
Gulianello
Michael
M
De Lombaert
Stéphane
S
Brodbeck
Robbin
R
Kieltyka
Andrzej
A
Hodgetts
Kevin J
KJ
D001665:Binding Sites; D015195:Drug Design; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000099052:CRF Receptor, Type 1
D011743:Pyrimidines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1