Daniel R. McMasters
United States Military Academy
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Featured researches published by Daniel R. McMasters.
Bioorganic & Medicinal Chemistry Letters | 2003
Christopher S. Burgey; Kyle A. Robinson; Terry A. Lyle; Philippe G. Nantermet; Harold G. Selnick; Richard C.A. Isaacs; S.Dale Lewis; Bobby J. Lucas; Julie A. Krueger; Rominder Singh; Cynthia Miller-Stein; Rebecca B. White; Bradley K. Wong; Elizabeth A. Lyle; Maria T. Stranieri; Jacquelynn J. Cook; Daniel R. McMasters; Janetta M. Pellicore; Swati Pal; Audrey A. Wallace; Franklin C. Clayton; Dennis L. Bohn; Denise C. Welsh; Joseph J. Lynch; Youwei Yan; Zhongguo Chen; Lawrence Kuo; Stephen J. Gardell; Jules A. Shafer; Joseph P. Vacca
In this manuscript we demonstrate that a modification principally directed toward the improvement of the aqueous solubility (i.e., introduction a P3 pyridine N-oxide) of the previous lead compound afforded a new series of potent orally bioavailable P1 N-benzylamide thrombin inhibitors. An expedited investigation of the P1 SAR with respect to oral bioavailability, plasma half-life, and human liver microsome stability revealed 5 as the best candidate for advanced evaluation.
Bioorganic & Medicinal Chemistry Letters | 2003
Kenneth E. Rittle; James C. Barrow; Kellie J. Cutrona; Kristen L Glass; Julie A. Krueger; Lawrence C. Kuo; S.Dale Lewis; Bobby J. Lucas; Daniel R. McMasters; Matthew M. Morrissette; Philippe G. Nantermet; Christina L. Newton; William M. Sanders; Youwei Yan; Joseph P. Vacca; Harold G. Selnick
Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the alpha-thrombin-hirugen complex provides an explanation for these unanticipated results.
Bioorganic & Medicinal Chemistry Letters | 2003
Philippe G. Nantermet; James C. Barrow; Christina L. Newton; Janetta M. Pellicore; MaryBeth Young; S.Dale Lewis; Bobby J. Lucas; Julie A. Krueger; Daniel R. McMasters; Youwei Yan; Lawrence C. Kuo; Joseph P. Vacca; Harold G. Selnick
A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of specific functional groups in the tether that enhanced functional activity against thrombin and provided exquisite selectivity against trypsin and tPA. X-ray crystallography and molecular modeling studies revealed the inhibitor-enzyme interactions responsible for this selectivity.
Bioorganic & Medicinal Chemistry Letters | 2008
Richard C.A. Isaacs; Mark G. Solinsky; Kellie J. Cutrona; Christina L. Newton; Adel M. Naylor-Olsen; Daniel R. McMasters; Julie A. Krueger; S.Dale Lewis; Bobby J. Lucas; Lawrence C. Kuo; Youwei Yan; J.J. Lynch; Elizabeth A. Lyle
Guided by X-ray crystallography of thrombin-inhibitor complexes and molecular modeling, alkylation of the N1 nitrogen of the imidazole P1 ligand of the pyridinoneacetamide thrombin inhibitor 1 with various acetamide moieties furnished inhibitors with significantly improved thrombin potency, trypsin selectivity, functional in vitro anticoagulant potency and in vivo antithrombotic efficacy. In the pyrazinoneacetamide series, oral bioavailability was also improved.
Bioorganic & Medicinal Chemistry Letters | 2011
Richard C.A. Isaacs; Christina L. Newton; Kellie J. Cutrona; Swati P. Mercer; Linda S. Payne; Kenneth J. Stauffer; Peter D. Williams; Jacquelynn J. Cook; Julie A. Krueger; S.Dale Lewis; Bobby J. Lucas; Elizabeth A. Lyle; Joseph J. Lynch; Daniel R. McMasters; Adel M. Naylor-Olsen; Maria T. Michener; Audrey A. Wallace
A novel 1,3,5-trisubstituted benzamide thrombin inhibitor template was designed via hybridization of a known aminopyridinoneacetamide and a known 1,3,5-trisubstituted phenyl ether. Optimization of this lead afforded a novel potent series of biaryl 1,3,5-trisubstituted benzenes with excellent functional anticoagulant potency.
Bioorganic & Medicinal Chemistry Letters | 2006
Ian M. Bell; Rodney A. Bednar; John F. Fay; Steven N. Gallicchio; Jerome H. Hochman; Daniel R. McMasters; Cynthia Miller-Stein; Eric L. Moore; Scott D. Mosser; Nicole T. Pudvah; Amy G. Quigley; Christopher A. Salvatore; Craig A. Stump; Cory R. Theberge; Bradley K. Wong; C. Blair Zartman; Xufang Zhang; Stefanie A. Kane; Samuel L. Graham; Joseph P. Vacca; Theresa M. Williams
Bioorganic & Medicinal Chemistry Letters | 2004
Philippe G. Nantermet; James C. Barrow; Stacey R. Lindsley; MaryBeth Young; Shi-Shan Mao; Steven S. Carroll; Carolyn Bailey; Michele Bosserman; Dennis Colussi; Daniel R. McMasters; Joseph P. Vacca; Harold G. Selnick
Bioorganic & Medicinal Chemistry Letters | 2005
James Z. Deng; Daniel R. McMasters; P.M Rabbat; Peter D. Williams; Craig A. Coburn; Youwei Yan; Lawrence Kuo; Lewis Sd; Bobby J. Lucas; Julie A. Krueger; B Strulovici; Joseph P. Vacca; Terry A. Lyle; Christopher S. Burgey
Bioorganic & Medicinal Chemistry Letters | 2004
Matthew M. Morrissette; Kenneth J. Stauffer; Peter D. Williams; Terry A. Lyle; Joseph P. Vacca; Julie A. Krueger; S.Dale Lewis; Bobby J. Lucas; Bradley K. Wong; Rebecca B. White; Cynthia Miller-Stein; Elizabeth A. Lyle; Audrey A. Wallace; Yvonne M. Leonard; Denise C. Welsh; Joseph J. Lynch; Daniel R. McMasters
Bioorganic & Medicinal Chemistry | 2006
Donnette D. Staas; Kelly L. Savage; Vanessa Sherman; Heidi L. Shimp; Terry A. Lyle; Lekhanh O. Tran; Catherine M. Wiscount; Daniel R. McMasters; Philip E.J. Sanderson; Peter D. Williams; Bobby J. Lucas; Julie A. Krueger; S.Dale Lewis; Rebecca B. White; Sean Yu; Bradley K. Wong; Christopher J. Kochansky; M. Reza Anari; Youwei Yan; Joseph P. Vacca