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

L W Hsin; E L Webster; G P Chrousos; P W Gold; W C Eckelman; C Contoreggi; K C Rice

doi:10.1016/s0960-894x(00)00071-8

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.

Authors

L W Hsin¹, E L Webster, G P Chrousos, P W Gold, W C Eckelman, C Contoreggi, K C Rice

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.

Publication types

Research Support, U.S. Gov't, P.H.S.

MeSH terms

Animals
Cerebellum / metabolism
Contrast Media / chemical synthesis*
Contrast Media / metabolism
Contrast Media / pharmacology*
Fluorine / chemistry
Pyrimidines / chemical synthesis*
Pyrimidines / metabolism
Pyrimidines / pharmacology*
Pyrroles / chemistry
Radioligand Assay
Rats
Receptors, Corticotropin-Releasing Hormone / metabolism*
Tomography, Emission-Computed

Substances

Contrast Media
Pyrimidines
Pyrroles
Receptors, Corticotropin-Releasing Hormone
Fluorine