Usa Reilly
Pfizer
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Publication
Featured researches published by Usa Reilly.
Journal of Medicinal Chemistry | 2012
Justin Ian Montgomery; Matthew Frank Brown; Usa Reilly; Loren M. Price; Joseph A. Abramite; Rose Barham; Ye Che; Jinshan Michael Chen; Seung Won Chung; E.M Collantes; Charlene R. Desbonnet; M Doroski; Jonathan L. Doty; J.J Engtrakul; Thomas M. Harris; Michael D. Huband; John D. Knafels; Karen L. Leach; Shenping Liu; Anthony Marfat; Laura A. McAllister; Eric McElroy; Carol A. Menard; Mark J. Mitton-Fry; Lisa Mullins; Mark C. Noe; J O'Donnell; Robert M. Oliver; Joseph Penzien; Mark Stephen Plummer
The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-negative antibacterial activity to comparator agents.
Journal of Medicinal Chemistry | 2009
Thomas V. Magee; Sharon L. Ripp; Bryan Li; Richard A. Buzon; Lou Chupak; Thomas J. Dougherty; Steven M. Finegan; Dennis Girard; Anne E. Hagen; Michael J. Falcone; Kathleen A. Farley; Karl Granskog; Joel R. Hardink; Michael D. Huband; Barbara J. Kamicker; Takushi Kaneko; Michael J. Knickerbocker; Jennifer Liras; Andrea Marra; Ivy Medina; Thuy-Trinh Nguyen; Mark C. Noe; R. Scott Obach; John P. O’Donnell; Joseph Penzien; Usa Reilly; John Schafer; Yue Shen; Gregory G. Stone; Timothy J. Strelevitz
Respiratory tract bacterial strains are becoming increasingly resistant to currently marketed macrolide antibiotics. The current alternative telithromycin (1) from the newer ketolide class of macrolides addresses resistance but is hampered by serious safety concerns, hepatotoxicity in particular. We have discovered a novel series of azetidinyl ketolides that focus on mitigation of hepatotoxicity by minimizing hepatic turnover and time-dependent inactivation of CYP3A isoforms in the liver without compromising the potency and efficacy of 1.
Bioorganic & Medicinal Chemistry Letters | 2013
Mark J. Mitton-Fry; Steven J. Brickner; Judith C. Hamel; Lori Brennan; Jeffrey M. Casavant; Michael Chen; Tao Chen; Xiaoyuan Ding; James P. Driscoll; Joel R. Hardink; Thuy Hoang; Erbing Hua; Michael D. Huband; Meghan Maloney; Anthony Marfat; Sandra P. McCurdy; Dale McLeod; Michael Plotkin; Usa Reilly; Shaughn Robinson; John Schafer; Richard M. Shepard; James F. Smith; Gregory G. Stone; Chakrapani Subramanyam; Kwansik Yoon; Wei Yuan; Richard P. Zaniewski; Christopher Zook
A structurally novel set of inhibitors of bacterial type II topoisomerases with potent in vitro and in vivo antibacterial activity was developed. Dual-targeting ability, hERG inhibition, and pharmacokinetic properties were also assessed.
Bioorganic & Medicinal Chemistry Letters | 2012
Laura A. McAllister; Justin Ian Montgomery; Joseph A. Abramite; Usa Reilly; Matthew Frank Brown; Jinshan M. Chen; Rose Barham; Ye Che; Seung Won Chung; Carol A. Menard; Mark J. Mitton-Fry; Lisa Mullins; Mark C. Noe; John P. O’Donnell; Robert M. Oliver; Joseph Penzien; Mark Stephen Plummer; Loren M. Price; Veerabahu Shanmugasundaram; Andrew P. Tomaras; Daniel P. Uccello
The synthesis and antibacterial activity of heterocyclic methylsulfone hydroxamates is presented. Compounds in this series are potent inhibitors of the LpxC enzyme, a key enzyme involved in the production of lipopolysaccharide (LPS) found in the outer membrane of Gram-negative bacteria. SAR evaluation of compounds in this series revealed analogs with potent antibacterial activity against challenging Gram-negative species such as Pseudomonas aeruginosa and Klebsiella pneumoniae.
Bioorganic & Medicinal Chemistry Letters | 2017
Mark J. Mitton-Fry; Steven J. Brickner; Judith C. Hamel; Rose Barham; Lori Brennan; Jeffrey M. Casavant; Xiaoyuan Ding; Steven M. Finegan; Joel R. Hardink; Thuy Hoang; Michael D. Huband; Meghan Maloney; Anthony Marfat; Sandra P. McCurdy; Dale McLeod; Chakrapani Subramanyam; Michael Plotkin; Usa Reilly; John Schafer; Gregory G. Stone; Daniel P. Uccello; Todd Wisialowski; Kwansik Yoon; Richard P. Zaniewski; Christopher Zook
Novel (non-fluoroquinolone) inhibitors of bacterial type II topoisomerases (NBTIs) are an emerging class of antibacterial agents. We report an optimized series of cyclobutylaryl-substituted NBTIs. Compound 14 demonstrated excellent activity both in vitro (S. aureus MIC90=0.125μg/mL) and in vivo (systemic and tissue infections). Enhanced inhibition of Topoisomerase IV correlated with improved activity in S. aureus strains with mutations conferring resistance to NBTIs. Compound 14 also displayed an improved hERG IC50 of 85.9μM and a favorable profile in the anesthetized guinea pig model.
Magnetic Resonance in Chemistry | 2017
Kathleen A. Farley; Usa Reilly; Dennis P. Anderson; Brian P. Boscoe; Mark W. Bundesmann; David A. Foley; Manjinder S. Lall; Chao Li; Matthew R. Reese; Jiangli Yan
In situ reaction monitoring tools offer the ability to track the progress of a synthetic reaction in real time to facilitate reaction optimization and provide kinetic/mechanistic insight. Herein, we report the utilization of flow NMR, flow IR, and other off‐line spectroscopy tools to monitor the progress of a flow chemistry reaction. The on‐line and off‐line tools were selected to facilitate the stereoselective kinetic resolution of a key racemic monomer, which lacked a chromophore, making conventional reaction monitoring difficult. Copyright
Archive | 2010
Matthew Frank Brown; Ye Che; Anthony Marfat; Michael Joseph Melnick; Justin Ian Montgomery; Usa Reilly
Archive | 2012
Usa Reilly; Michael Joseph Melnick; Matthew Frank Brown; Mark Stephen Plummer; Justin Ian Montgomery; Ye Che; Loren M. Price
Bioorganic & Medicinal Chemistry Letters | 2007
Kevin Daniel Freeman-Cook; Lawrence A. Reiter; Mark C. Noe; Amy S. Antipas; Dennis E. Danley; Kaushik Datta; James T. Downs; Shane Allen Eisenbeis; James D. Eskra; David J. Garmene; Elaine M. Greer; Richard J. Griffiths; Roberto E. Guzman; Joel R. Hardink; Fouad Janat; Christopher S. Jones; Gary J. Martinelli; Peter G. Mitchell; Ellen R. Laird; Jennifer Liras; Lori L. Lopresti-Morrow; Jayvardhan Pandit; Usa Reilly; Donald G. Robertson; Marcie L. Vaughn-Bowser; Lilli A. Wolf-Gouviea; Sue A. Yocum
Archive | 2012
Joseph A. Abramite; Matthew Frank Brown; Jinshan Michael Chen; Michael Joseph Melnick; Justin Ian Montgomery; Usa Reilly