David N. Deaton

GlaxoSmithKline (United States)

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i-10 index

Research Trends

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Co-Authors

Aaron B. Miller

Research Triangle Park Foundation

Larry R. Miller

National Institute of Arthritis and Musculoskeletal and Skin Diseases

Lois L. Wright

GlaxoSmithKline (United Kingdom)

Lisa M. Shewchuk

South College

Robert B. McFadyen

Research Triangle Park Foundation

Anne M. Hassell

Research Triangle Park Foundation

Derril H. Willard

Research Triangle Park Foundation

David G. Barrett

Eli Lilly (United States)

John G. Catalano

Research Triangle Park Foundation

Stacey T. Long

GlaxoSmithKline (United States)

Cooperative Institutions

GlaxoSmithKline (United States)

137

Research Triangle Park Foundation

128

GlaxoSmithKline (United Kingdom)

GlaxoSmithKline (Netherlands)

South College

University of Pennsylvania

Duke University

University of North Carolina at Chapel Hill

Georgetown University

Cleveland Clinic

Author Statistics

Papers

Citation

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The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors

Bioorganic & Medicinal Chemistry (2019)

David N. Deaton Young Do Jason A. Holt Michael R. Jeune Henning F. Kramer

Quinoline

IC50

ADME

Moiety

Prostaglandin D2

10.1016/j.bmc.2019.02.017

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Citations (18)

Cathepsin K complexed with t-butyl(1S)-1-cyclohexyl-2-oxoethylcarbamate

John G. Catalano David N. Deaton Eric S. Furfine Anne M. Hassell Robert B. McFadyen

10.2210/pdb1q6k/pdb

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Citations (0)

Potent and selective P2–P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1′, P1, and/or P3 substitutions

Bioorganic & Medicinal Chemistry Letters (2004)

David G. Barrett John G. Catalano David N. Deaton Anne M. Hassell Stacey T. Long

Cysteine protease

Cathepsin K

Cysteine Proteinase Inhibitors

Cathepsin S

Molecular model

Cathepsin L

10.1016/j.bmcl.2004.07.031

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Citations (26)

Synthesis of (+)-dihydrocompactin and (+)-compactin via vinylsilane terminated cationic cyclization

Tetrahedron Letters (1991)

Steven D. Burke David N. Deaton

Vinylsilane

Polyene

Cationic polymerization

10.1016/s0040-4039(00)92272-x

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Citations (28)

Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead

Bioorganic & Medicinal Chemistry Letters (2008)

David L. Carlton Lissa J. Collin-Smith Alejandro J. Daniels David N. Deaton Aaron S. Goetz

Thioether

Moiety

Lead compound

10.1016/j.bmcl.2008.09.033

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Citations (18)

Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38

Journal of Medicinal Chemistry (2015)

J. David Becherer Eric E. Boros Tiffany Carpenter David J. Cowan David N. Deaton

Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure-activity relationships (SAR) of the 4-, 6-, and 8-substituents of the quinoline ring resulted in the identification of approximately 10-100-fold more potent human CD38 inhibitors. Several of these molecules also exhibited pharmacokinetic parameters suitable for in vivo animal studies, including low clearances and decent oral bioavailability. Two of these CD38 inhibitors, 1ah and 1ai, were shown to elevate NAD tissue levels in liver and muscle in a diet-induced obese (DIO) C57BL/6 mouse model. These inhibitor tool compounds will enable further biological studies of the CD38 enzyme as well as the investigation of the therapeutic implications of NAD enhancement in disease models of abnormally low NAD.

Quinoline

Carboxamide

10.1021/acs.jmedchem.5b00992

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Citations (46)

Cathepsin K complexed with a constrained ketoamide inhibitor

David G. Barrett Virginia M. Boncek John G. Catalano David N. Deaton Anne M. Hassell

10.2210/pdb1yt7/pdb

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Citations (0)

Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors

Journal of Medicinal Chemistry (2015)

Curt D. Haffner J. David Becherer Eric E. Boros Rodolfo Cadilla Tiffany Carpenter

A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasma, liver, and muscle tissue. In particular, compound 78c was given to diet induced obese (DIO) C57Bl6 mice, elevating NAD > 5-fold in liver and >1.2-fold in muscle versus control animals at a 2 h time point. The compounds described herein possess the most potent CD38 inhibitory activity of any small molecules described in the literature to date. The inhibitors should allow for a more detailed assessment of how NAD elevation via CD38 inhibition affects physiology in NAD deficient states.

10.1021/jm502009h

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Citations (115)

Effect of matrix metalloproteinase inhibitors on tumor growth and spontaneous metastasis

Clinical & Experimental Metastasis (1996)

James G. Conway Suzanne J. Trexler Jean A. Wakefield Brian E. Marron David L. Emerson

Primary tumor

Matrix metalloproteinase inhibitor

10.1007/bf00121208

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Citations (32)

Human CD38 complexed with inhibitor 2 [4-[(2,6-dimethylbenzyl)amino]-2-methylquinoline-8-carboxamide]

Lisa M. Shewchuk David N. Deaton Eugene L. Stewart

Carboxamide

10.2210/pdb4xjt/pdb

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Citations (0)