Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: The development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor

A series of fluoro-substituted 4-(dialkylamino)pyrrolo[2,3-d]pyrimidines was synthesized and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 11a and 11b possessed very high CRHR1 affinity (Ki=3.5, 0.91 nM, respectively). They are promisi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.707-710
Hauptverfasser:	HSIN, L.-W, WEBSTER, E. L, CHROUSOS, G. P, GOLD, P. W, ECKELMAN, W. C, CONTOREGGI, C, RICE, K. C
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cerebellum - metabolism Contrast Media - chemical synthesis Contrast Media - metabolism Contrast Media - pharmacology Fluorine - chemistry Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - metabolism Pyrimidines - pharmacology Pyrroles - chemistry Radioligand Assay Rats Receptors, Corticotropin-Releasing Hormone - metabolism Tomography, Emission-Computed
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Zusammenfassung:	A series of fluoro-substituted 4-(dialkylamino)pyrrolo[2,3-d]pyrimidines was synthesized and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 11a and 11b possessed very high CRHR1 affinity (Ki=3.5, 0.91 nM, respectively). They are promising candidates for the development of 18F-containing nonpeptide PET radioligands for CRHR1.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/s0960-894x(00)00071-8