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 |
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| Authors: | Hsin L W Webster E L Chrousos G P Gold P W Eckelman W C Contoreggi C Rice K C |
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| Institution: | Laboratory of Medicinal Chemistry, NIDDK, NIH, Bethesda, MD 20892, USA. |
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| Abstract: | A series of fluoro-substituted 4-(dialkylamino)pyrrolo2,3-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. |
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