Synthesis and biological activity of fluoro-substituted pyrrolo [2, 3-d] pyrimidines: the development of potential positron emission tomography imaging agents for the …

…, PW Gold, WC Eckelman, C Contoreggi…

文献索引：Hsin, Ling-Wei; Webster, Elizabeth L.; Chrousos, George P.; Gold, Philip W.; Eckelman, William C.; Contoreggi, Carlo; Rice, Kenner C. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 8 p. 707 - 710

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被引用次数: 23

摘要

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.