Zobrazeno 1 - 10
of 30
pro vyhledávání: '"David D. Davey"'
Autor:
Amy Liang, Dao Lentz, Bin Ye, David D. Davey, Karen May, John Parkinson, Beverly King, Hong Ye, Gary Phillips, Robert G. Wei, William J. Guilford, Sabine Schlyer, Lisa M. Mendoza, Selchau Victor, Seock-Kyu Khim, Jih-Lie Tseng, John G. Bauman, Kochanny Monica, Thomas A. Kirkland, Ming Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3891-3894
The synthesis and biological evaluation of a series of N-alkyl glycine amide analogs as LTA(4)-h inhibitors and the importance of the introduction of a benzoic acid group to the potency and pharmacokinetic parameters of our analogs are described. The
Autor:
Marc Adler, Wei Xu, Sunil K. Koovakkat, Eric Pham, Marc Whitlow, Qinglan Huang, David D. Davey, John Parkinson, Gary Phillips, Shendong Yuan, Mark A. Polokoff
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2505-2508
A series of compounds was rationally designed as inhibitors of dimer formation of the inducible isoform of nitric oxide synthase, and subsequent nitric oxide production. The conformation of two fragments obtained from a crystal structure was utilized
Autor:
Jih-Lie Tseng, David D. Davey, Mark A. Polokoff, Gary Phillips, Raju Mohan, Marc Whitlow, Shendong Yuan, Marc Adler, Robert G. Wei, Elena Ho, Wei Xu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2499-2504
A new series of 1-(1,3-benzodioxol-5-ylmethyl)-3-[4-(1H-Imidazol-1-yl)phenoxy]-piperidine analogs were designed and identified as potent and selective inhibitors of NO formation based both on the crystal structure of a murine iNOS Δ114 monomer domai
Autor:
Damian Arnaiz, Gary Phillips, Shawn David Erickson, Marc Whitlow, Margaret Kenrick, James J. Devlin, Gonghua Pan, Cecile Santos, William J. Guilford, Robert G. Wei, Marc Adler, Kurt W. Saionz, Bin Ye, Ron Vergona, John Parkinson, Zuchun Spring Zhao, David D. Davey, Michael Ohlmeyer, Babu Subramanyam, Vidyadhar M. Paradkar, Mark A. Polokoff, Keith A. Eagen, Michael M. Morrissey
Publikováno v:
Journal of Medicinal Chemistry. 50:1146-1157
By the screening of a combinatorial library for inhibitors of nitric oxide (NO) formation by the inducible isoform of nitric oxide synthase (iNOS) using a whole-cell assay, 2-(imidazol-1-yl)pyrimidines were identified. Compounds were found to inhibit
Autor:
Sunil K. Koovakkat, Brad O. Buckman, Keith Eagen, Shung Wu, Ng Howard P, Raju Mohan, Wei Xu, Elena Ho, Lan Trinh, Babu Subramanyam, Meg McCarrick, Gary Phillips, Morrissey Michael M, Michael Pinkerton, William J. Guilford, Marc Whitlow, Amy Liang, David D. Davey
Publikováno v:
Journal of Medicinal Chemistry. 45:2484-2493
A novel series of diaryloxypyridines have been designed as selective nanomolar factor Xa (fXa) inhibitors for use as anticoagulants. In this paper, we describe our efforts to identify an additional interaction and a replacement for the distal amidine
Autor:
Marc Whitlow, Sung-Hou Kim, Jarmila Jancarik, David D. Davey, David R. Light, Marc Adler, Gary Phillips, Galina Rumennik
Publikováno v:
Biochemistry. 39:12534-12542
Factor Xa plays a critical role in the formation of blood clots. This serine protease catalyzes the conversion of prothrombin to thrombin, the first joint step that links the intrinsic and extrinsic coagulation pathways. There is considerable interes
Autor:
Sunil K. Koovakkat, William J. Guilford, Wei Xu, Brad O. Buckman, Marian Seto, Brain Griedel, David R. Light, Morrissey Michael M, David D. Davey, Kenneth J. Shaw, Damain O. Arnaiz, Amy Liang, Gary Phillips, Zuchun Zhao, Raju Mohan, Marc Whitlow
Publikováno v:
Acta Crystallographica Section D Biological Crystallography. 55:1395-1404
Factor Xa is a serine protease which activates thrombin (factor IIa) and plays a key regulatory role in the blood-coagulation cascade. Factor Xa is, therefore, an important target for the design of anti-thrombotics. Both factor Xa and thrombin share
Autor:
Joseph Post, Elena Ho, Amy Liang, Ron Vergona, Raju Mohan, Lan Trinh, Marc Whitlow, Janette Walters, Morrissey Michael M, Wei Xu, Josephine Hinchman, Sunil K. Koovakkat, David D. Davey, Gary Phillips, David R. Light, Brad O. Buckman, William J. Guilford, David J. Smith, Kathy White, Mark E. Sullivan, Keith Eagen, Shung Wu, Ng Howard P, Babu Subramanyam, Kenneth J. Shaw
Publikováno v:
Journal of Medicinal Chemistry. 41:3557-3562
Autor:
Brian D. Griedel, Keith Eagen, Shung C. Wu, Morrissey Michael M, Yuo-Ling Chou, Karna Lyn Sacchi, Lan Trinh, David D. Davey, Kenneth J. Shaw, Karanjawala Rushad E, Dao Lentz, Kochanny Monica, Amy Liang, Gary Phillips
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(3)
Compound 1 was identified by high throughput screening as a novel, potent, non-amidine factor Xa inhibitor with good selectivity against thrombin and trypsin. A series of modifications of the three aromatic groups of 1 was investigated. Substitution
Autor:
Kirk Mcmillan, Gonghua Pan, Michael M. Morrissey, Leslie J. Browne, Mark A. Polokoff, Baldwin John J, Ronald Vergona, Gary Phillips, Marc Adler, Michael Ohlmeyer, David D. Davey, John Parkinson, Cornell Mallari, Charles B. Glaser, Nolan H. Sigal, Shawn David Erickson, Keith A. Eagen, James J. Devlin, Tish A. Young, Ronald E. Dolle, Eric Blasko, Daniel Chelsky, Richard I. Feldman, Douglas S. Auld, Marc Whitlow
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America. 97(4)
Potent and selective inhibitors of inducible nitric oxide synthase (iNOS) (EC 1.14.13.39 ) were identified in an encoded combinatorial chemical library that blocked human iNOS dimerization, and thereby NO production. In a cell-based iNOS assay (A-172