Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371035 | Bioorganic & Medicinal Chemistry Letters | 2015 | 4 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sean R. Bollinger, Darren W. Engers, Elizabeth A. Ennis, Jane Wright, Charles W. Locuson, Craig W. Lindsley, Randy D. Blakely, Corey R. Hopkins,