Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging

被引：6

作者：

Davison, Holly R. ^{[1
]}

Solano, Danielle M. ^{[1
]}

Phuan, Puay-Wah ^{[2
,3
]}

Verkman, A. S. ^{[2
,3
]}

Kurth, Mark J. ^{[1
]}

机构：

[1] Univ Calif Davis, Dept Chem, Davis, CA 95616 USA

[2] Univ Calif San Francisco, Dept Med, San Francisco, CA 94143 USA

[3] Univ Calif San Francisco, Dept Physiol, San Francisco, CA 94143 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 04期

基金：

美国国家卫生研究院; 美国国家科学基金会;

关键词：

Cystic fibrosis; PET; Corrector; Potentiator; Delta F508-CFTR; TRANSMEMBRANE CONDUCTANCE REGULATOR; SMALL-MOLECULE CORRECTORS; EMISSION-TOMOGRAPHY PET; CYSTIC-FIBROSIS; CFTR;

D O I：

10.1016/j.bmcl.2011.12.128

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

F-19-modified bithiazole correctors and phenylglycine potentiators of the Delta F508-CFTR chloride channel were synthesized and their function assayed in cells expressing human Delta F508-CFTR and a halide-sensitive fluorescent protein. Fluorine was incorporated into each scaffold using prosthetic groups for future biodistribution imaging studies using positron emission tomography (PET). The Delta F508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds. (C) 2011 Elsevier Ltd. All rights reserved.

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页码：1602 / 1605

页数：4

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