Synthesis of 3-phenylpyrazolo[4,3- b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-Releasing factor receptor type-1 antagonists

3-Phenylpyrazolo[4,3- b]pyridines were synthesized via a cyclization of 4-amino-3-phenylpyrazoles 11– 13 with ethyl acetoacetate. These compounds were found to be potent CRF 1 antagonists. The 2-alkylpyrazolo[4,3- b]pyridines were more polar but less active than the corresponding 1-alkyl-isomers. Gr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (19), p.3367-3370
Hauptverfasser:	Wilcoxen, Keith, Huang, Charles Q, McCarthy, James R, Grigoriadis, Dimitri E, Chen, Chen
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Humans Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrazoles - chemical synthesis Pyrazoles - pharmacology Pyridines - chemical synthesis Pyridines - pharmacology Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Receptors, Corticotropin-Releasing Hormone - metabolism Structure-Activity Relationship
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Zusammenfassung:	3-Phenylpyrazolo[4,3- b]pyridines were synthesized via a cyclization of 4-amino-3-phenylpyrazoles 11– 13 with ethyl acetoacetate. These compounds were found to be potent CRF 1 antagonists. The 2-alkylpyrazolo[4,3- b]pyridines were more polar but less active than the corresponding 1-alkyl-isomers. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00621-8