Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones.

Derek J Denhart,Dmitry Zuev,Jonathan L Ditta,Richard A Hartz,Vijay T Ahuja,Ronald J Mattson,Hong Huang,Gail K Mattson,Larisa Zueva,Julia M Nielsen,Edward S Kozlowski,Nicholas J Lodge,Joanne J Bronson,John E Macor

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

A series of pyrazinones were prepared and evaluated as potential CRF1R PET imaging agents. Optimization of their CRF1R binding potencies and octanol–phosphate buffer phase distribution coefficients is discussed herein.

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关键词

CRF,PET,Depression,Pyrazinones,Fluoroalkyl

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