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Dive into the research topics where Mark R. Rauckhorst is active.

Publication


Featured researches published by Mark R. Rauckhorst.


Organic Letters | 2009

One-Pot Synthesis of N-Arylpyrazoles from Arylhalides

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

5-(2-Pyrimidinyl)-imidazo[1,2-a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV

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

Siderophore Receptor-Mediated Uptake of Lactivicin Analogues in Gram-Negative Bacteria

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

The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents

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

Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.

Jeffrey W. Corbett; Mark R. Rauckhorst; Fang Qian; Robert L. Hoffman; Christopher S. Knauer; Lawrence W. Fitzgerald


Archive | 2002

N-azabicyclo-substituted hetero-bicyclic carboxamides as nachr agonists

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

N-(azabicyclo moieties)-substituted hetero-bicyclic aromatic compounds for the treatment of disease

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

Quinuclidine-substituted heteroaromatic compounds as ligands at nicotinic acetylcholine receptors

Daniel P. Walker; Donn G. Wishka; Jeffrey W. Corbett; Mark R. Rauckhorst; David W. Piotrowski; Vincent E. Groppi


Synfacts | 2009

One-Pot Synthesis of N -Arylpyrazoles from Aryl Halides

Brian S. Gerstenberger; Mark R. Rauckhorst; Jeremy T. Starr


Synfacts | 2009

One-Pot Synthesis of N-Arylpyrazolesfrom Aryl Halides

Brian S. Gerstenberger; Mark R. Rauckhorst; Jeremy T. Starr

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