Potential CRF 1 R PET imaging agents: N-Fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2, 7-dimethyl-N-alkylpyrazolo [1, 5-a][1, 3, 5] triazin-4-amines

…, L Zueva, JM Nielsen, ES Kozlowski, XS Huang…

Index: Zuev, Dmitry; Mattson, Ronald J.; Huang, Hong; Mattson, Gail K.; Zueva, Larisa; Nielsen, Julia M.; Kozlowski, Edward S.; Huang, Xiaohua Stella; Wu, Dedong; Gao, Qi; Lodge, Nicholas J.; Bronson, Joanne J.; MacOr, John E. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2484 - 2488

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Citation Number: 14

Abstract

A series of N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2, 7-dimethyl-N-alkylpyrazolo [1, 5-a][1, 3, 5] triazin-4-amines were prepared and evaluated as potential CRF1R PET imaging agents. Optimization of their CRF1R binding potencies and octanol–phosphate buffer phase distribution coefficients resulted in discovery of analog 7e (IC50= 6.5 nM, logD= 3.5).