A
Aaron C. Smith
Researcher at Pfizer
Publications - 37
Citations - 1018
Aaron C. Smith is an academic researcher from Pfizer. The author has contributed to research in topics: AMPK & Lactam. The author has an hindex of 13, co-authored 36 publications receiving 829 citations.
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Journal ArticleDOI
Palladium-catalyzed sulfination of aryl and heteroaryl halides: direct access to sulfones and sulfonamides.
TL;DR: This reaction operates under mild conditions and provides access to a wide range of aryl and heteroaryl sulfinates, a useful and versatile class of synthetic intermediates, and one-pot protocols allowing direct access to sulfones and sulfonamides have been developed.
Journal ArticleDOI
Palladium‐Catalyzed Synthesis of (Hetero)Aryl Alkyl Sulfones from (Hetero)Aryl Boronic Acids, Unactivated Alkyl Halides, and Potassium Metabisulfite
TL;DR: A stoichiometric experiment has led to the isolation of a catalytically active dimeric palladium sulfinate complex, which was characterized by X-ray diffraction analysis.
Journal ArticleDOI
Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms
Matthew F. Calabrese,Francis Rajamohan,Melissa S. Harris,Nicole Caspers,Rachelle Magyar,Jane M. Withka,Hong Wang,Kris A. Borzilleri,Parag Sahasrabudhe,Lise R. Hoth,Kieran F. Geoghegan,Seungil Han,Janice A. Brown,Timothy A. Subashi,Allan R. Reyes,Richard K. Frisbie,Jessica Ward,Russell A. Miller,James A. Landro,Allyn T. Londregan,Philip A. Carpino,Shawn Cabral,Aaron C. Smith,Edward L. Conn,Kimberly O. Cameron,Xiayang Qiu,Ravi G. Kurumbail +26 more
TL;DR: The full-length structure of the widely expressed α1β1γ1 isoform of mammalian AMPK is provided, along with detailed kinetic and biophysical characterization, and binding of the broadly studied synthetic activator A769662 and its analogs are characterized.
Journal ArticleDOI
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
Kimberly O. Cameron,Daniel W. Kung,Amit S. Kalgutkar,Ravi G. Kurumbail,Russell A. Miller,Christopher T. Salatto,Jessica Ward,Jane M. Withka,Samit Kumar Bhattacharya,Markus Boehm,Kris A. Borzilleri,Janice A. Brown,Matthew F. Calabrese,Nicole Caspers,Emily Cokorinos,Edward L. Conn,Matthew S. Dowling,David J. Edmonds,Heather Eng,Dilinie P. Fernando,Richard K. Frisbie,David Hepworth,James A. Landro,Yuxia Mao,Francis Rajamohan,Allan R. Reyes,Colin R. Rose,Tim F. Ryder,Andre Shavnya,Aaron C. Smith,Meihua Tu,Angela Wolford,Jun Xiao +32 more
TL;DR: Optimization of the core and aryl appendage improved oral absorption and culminated in the identification of indole acid, PF-06409577 (7), which was advanced to first-in-human trials for the treatment of diabetic nephropathy.
Journal ArticleDOI
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Roger B. Ruggeri,Leonard Buckbinder,Scott W. Bagley,Philip A. Carpino,Edward L. Conn,Matthew S. Dowling,Dilinie P. Fernando,Wenhua Jiao,Daniel W. Kung,Suvi T. M. Orr,Yingmei Qi,Benjamin N. Rocke,Aaron C. Smith,Joseph S. Warmus,Yan Zhang,Daniel Merritt Bowles,Daniel W. Widlicka,Heather Eng,Tim F. Ryder,Raman Sharma,Angela Wolford,Carlin Okerberg,Karen Walters,Tristan S. Maurer,Yanwei Zhang,Paul D. Bonin,Samantha N. Spath,Gang Xing,David Hepworth,Kay Ahn,Amit S. Kalgutkar +30 more
TL;DR: N1-Substituted-6-arylthiouracils exhibited low partition ratios and high selectivity for MPO over thyroid peroxidase and cytochrome P450 isoforms, and demonstrated inhibition of MPO activity in lipopolysaccharide-stimulated human whole blood.