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Updated: Aug 7, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors
Alexey Rivkin1, Yoona R Kim, Mark T Goulet
1Department of Chemistry, Merck Research Laboratories, Boston, MA 02115, USA. alexey_rivkin@merck.com
Abstract:
A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC(50) = 1.4 microM, SAR studies led to compounds with more than 70-fold increase in potency (IC(50) < 20 nM).
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