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Bioorg Med Chem. 2016 Apr 1;24(7):1455-68. doi: 10.1016/j.bmc.2016.02.006. Epub 2016 Feb 16.

Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.

Author information

1
Discovery Chemistry, Research and Development, Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA. Electronic address: louis.chupak@bms.com.
2
Discovery Chemistry, Research and Development, Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA.
3
Neuroscience Biology, Disease Sciences and Biologics, Research and Development, Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA.
4
Lead Evaluation, Discovery, Research and Development, Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA.
5
Discovery Chemistry Platforms, Research and Development, Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA.

Abstract

N-Benzylic-substituted glycine sulfonamides that reversibly inhibit diacylglycerol (DAG) lipases are reported. Detailed herein are the structure activity relationships, profiling characteristics and physico-chemical properties for the first reported series of DAG lipase (DAGL) inhibitors that function without covalent attachment to the enzyme. Highly potent examples are presented that represent valuable tool compounds for studying DAGL inhibition and constitute important leads for future medicinal chemistry efforts.

KEYWORDS:

2-Arachidonoylglycerol; Diacylglycerol; Endocannabinoid; Glycine; Lipase inhibitor; Sulfonamide

PMID:
26917221
DOI:
10.1016/j.bmc.2016.02.006
[Indexed for MEDLINE]

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