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Dive into the research topics where Daniel R. McMasters is active.

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Featured researches published by Daniel R. McMasters.


Bioorganic & Medicinal Chemistry Letters | 2003

Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.

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

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.

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

Design and synthesis of potent and selective macrocyclic thrombin inhibitors

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

Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.

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

Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.

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

Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.

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

Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P′1 group

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

Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.

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

Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability

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

Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability

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

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Bobby J. Lucas

United States Military Academy

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Joseph P. Vacca

United States Military Academy

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Julie A. Krueger

United States Military Academy

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S.Dale Lewis

United States Military Academy

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Youwei Yan

United States Military Academy

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Bradley K. Wong

United States Military Academy

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Christina L. Newton

United States Military Academy

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Philippe G. Nantermet

United States Military Academy

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Terry A. Lyle

United States Military Academy

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