@article{1035951179ac4d5dbe1e081095d09bce,
title = "Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter",
abstract = "The synthesis and SAR of 4-methoxy-3-(piperidin-4-yl) benzamides identified after a high-throughput screen of the MLPCN library is reported. SAR was explored around the 3-piperidine substituent as well as the amide functionality of the reported compounds. Starting from the initial lead compounds, 1-7, iterative medicinal chemistry efforts led to the identification of ML352 (10m). ML352 represents a potent and selective inhibitor of CHT based on a drug-like scaffold.",
keywords = "CHT, Choline transporter, ML352, MLPCN, Structure-activity relationship",
author = "Bollinger, {Sean R.} and Engers, {Darren W.} and Ennis, {Elizabeth A.} and Jane Wright and Locuson, {Charles W.} and Lindsley, {Craig W.} and Blakely, {Randy D.} and Hopkins, {Corey R.}",
note = "Funding Information: The authors would like to thank Mr. Ryan Morrison and Frank Byers for technical assistance with the PK experiments. Vanderbilt is a member of the MLPCN and houses the Vanderbilt Specialized Chemistry Center for Accelerated Probe Development. This work was generously supported by the NIH/MLPCN Grant U54 MH084659 (C.W.L.). In addition, this work was supported by CTSA award UL1TR000445 from the National Center for Advancing Translational Sciences (EAE), and NIH Awards GM07628 (EAE), MH073159 (RDB), and a Zenith Award from the Alzheimer{\textquoteright}s Foundation (RDB). Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd.All rights reserved.",
year = "2015",
month = apr,
day = "15",
doi = "10.1016/j.bmcl.2015.02.058",
language = "English (US)",
volume = "25",
pages = "1757--1760",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "8",
}