2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2000 Apr 17;10(8):707-10. doi: 10.1016/s0960-894x(00)00071-8.
L W Hsin 1,  E L Webster,  G P Chrousos,  P W Gold,  W C Eckelman,  C Contoreggi,  K C Rice
Affiliations

Affiliation

  • 1 Laboratory of Medicinal Chemistry, NIDDK, NIH, Bethesda, MD 20892, USA.
PMID: 10782669 DOI: 10.1016/s0960-894x(00)00071-8
Abstract

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.

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