Structure–activity relationships of novel iodinated quinoline-2-carboxamides for targeting the translocator protein†,10.1039/C3MD00249G

批量搜索

批量搜索

热搜：

Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

Structure–activity relationships of novel iodinated quinoline-2-carboxamides for targeting the translocator protein†

Adele Blair,Louise Stevenson,Deborah Dewar,Sally L. Pimlott,Andrew Sutherland

MedChemComm Pub Date : 09/17/2013 00:00:00 , DOI:10.1039/C3MD00249G

Abstract

In an effort to develop a new SPECT imaging agent for the translocator protein (TSPO), a series of novel iodinated quinoline-2-carboxamides have been synthesised and evaluated for binding affinity using rat brain homogenates. The outcome of the biological testing in combination with HPLC determination of the physicochemical properties of these compounds directed the design of new analogues resulting in 4-(2-iodophenyl)quinoline-2-N-diethylcarboxamide, a new TSPO ligand with higher affinity than the widely used clinical imaging agent PK11195.