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
  • 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.

Products