Mark R. Rauckhorst
Pfizer
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Publication
Featured researches published by Mark R. Rauckhorst.
Organic Letters | 2009
Brian S. Gerstenberger; Mark R. Rauckhorst; Jeremy T. Starr
A simple one-pot method for the synthesis of diversely functionalized pyrazoles from aryl nucleophiles, di-tert-butylazodicarboxlate, and 1,3-dicarbonyl or equivalent compounds is presented.
Bioorganic & Medicinal Chemistry Letters | 2009
Jeremy T. Starr; Richard John Sciotti; Debra Hanna; Michael D. Huband; Lisa Mullins; Hongliang Cai; Jeffrey W. Gage; Mandy Lockard; Mark R. Rauckhorst; Robert M. Owen; Manjinder S. Lall; Mark Tomilo; Huifen Chen; Sandra P. McCurdy; Michael R. Barbachyn
Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2-a]pyridine template exhibited MICs (microg/mL) of 0.06-64 (Sau), 0.25-64 (MRSA), 0.06-64 (Spy), 0.06-64 (Spn), and 0.03-64 (FQR Spn). Selected examples were efficacious in mouse sepsis and lung infection models at <50mg/kg (PO dosing).
Journal of Medicinal Chemistry | 2014
Jeremy T. Starr; Matthew Frank Brown; Lisa M. Aschenbrenner; Nicole Caspers; Ye Che; Brian S. Gerstenberger; Michael D. Huband; John D. Knafels; M. Megan Lemmon; Chao Li; Sandra P. McCurdy; Eric McElroy; Mark R. Rauckhorst; Andrew P. Tomaras; Jennifer A. Young; Richard P. Zaniewski; Veerabahu Shanmugasundaram; Seungil Han
Multidrug-resistant Gram-negative pathogens are an emerging threat to human health, and addressing this challenge will require development of new antibacterial agents. This can be achieved through an improved molecular understanding of drug-target interactions combined with enhanced delivery of these agents to the site of action. Herein we describe the first application of siderophore receptor-mediated drug uptake of lactivicin analogues as a strategy that enables the development of novel antibacterial agents against clinically relevant Gram-negative bacteria. We report the first crystal structures of several sideromimic conjugated compounds bound to penicillin binding proteins PBP3 and PBP1a from Pseudomonas aeruginosa and characterize the reactivity of lactivicin and β-lactam core structures. Results from drug sensitivity studies with β-lactamase enzymes are presented, as well as a structure-based hypothesis to reduce susceptibility to this enzyme class. Finally, mechanistic studies demonstrating that sideromimic modification alters the drug uptake process are discussed.
Bioorganic & Medicinal Chemistry Letters | 2007
Sean T. Murphy; Heather L. Case; Edmund L. Ellsworth; Susan Elizabeth Hagen; Michael D. Huband; Themis Joannides; Chris Limberakis; Keith R. Marotti; Amy M. Ottolini; Mark R. Rauckhorst; Jeremy T. Starr; Michael Andrew Stier; Clarke B. Taylor; Tong Zhu; Adrian Blaser; William A. Denny; Guo Liang Lu; Jeff B. Smaill; Freddy Rivault
Bioorganic & Medicinal Chemistry Letters | 2007
Jeffrey W. Corbett; Mark R. Rauckhorst; Fang Qian; Robert L. Hoffman; Christopher S. Knauer; Lawrence W. Fitzgerald
Archive | 2002
Daniel P. Walker; Eric Jon Jacobsen; David W. Piotrowski; Donn G. Wishka; Jeffrey W. Corbett; Vincent E. Groppi; Brad A. Acker; Mark R. Rauckhorst
Archive | 2002
Daniel P. Walker; Eric Jon Jacobsen; David W. Piotrowski; Brad A. Acker; Donn G. Wishka; Jeffrey W. Corbett; Mark R. Rauckhorst; Vincent E. Groppi
Archive | 2002
Daniel P. Walker; Donn G. Wishka; Jeffrey W. Corbett; Mark R. Rauckhorst; David W. Piotrowski; Vincent E. Groppi
Synfacts | 2009
Brian S. Gerstenberger; Mark R. Rauckhorst; Jeremy T. Starr
Synfacts | 2009
Brian S. Gerstenberger; Mark R. Rauckhorst; Jeremy T. Starr