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. The synthesis of a series...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-08, Vol.12 (16), p.2133-2136
Hauptverfasser:	Yuan, Jun, Gulianello, Michael, De Lombaert, Stéphane, Brodbeck, Robbin, Kieltyka, Andrzej, Hodgetts, Kevin J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Biological and medical sciences Drug Design Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00358-X