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. 2007 Sep 1;17(17):4882-5.
doi: 10.1016/j.bmcl.2007.06.043. Epub 2007 Jun 14.

Quinazoline derivatives as MC-I inhibitors: evaluation of myocardial uptake using Positron Emission Tomography in rat and non-human primate

Ajay Purohit  1 , Richard Benetti, Megan Hayes, Mary Guaraldi, Mikhail Kagan, Padmaja Yalamanchilli, Fran Su, Michael Azure, Mahesh Mistry, Ming Yu, Simon Robinson, Douglas D Dischino, David Casebier
Affiliations

Quinazoline derivatives as MC-I inhibitors: evaluation of myocardial uptake using Positron Emission Tomography in rat and non-human primate

Ajay Purohit et al. Bioorg Med Chem Lett. .

Abstract

Several quinazoline derivatives were made as mitochondrial complex 1 inhibitors. Compound 4 showed an IC(50) of 11.3 nM and was the most potent compound of this series. The (18)F analog of 4, [(18)F] 4, was injected in the rat and showed high and rapid heart uptake, fast liver clearance, and low blood uptake. Images obtained using a microPET showed clear delineation of the myocardium in normal rats and perfusion deficit in ischemic rats. In the non-human primate, [(18)F] 4 showed rapid uptake and clearance from the myocardium and high liver uptake.

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