Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Diem N Nguyen"'
Autor:
Ahmed R Aoun, Nagaraju Mupparapu, Diem N Nguyen, Tae Ho Kim, Christopher M. Nguyen, Zhengfeiyue Pan, Sherif I. Elshahawi
Publikováno v:
ChemCatChem
Indole is a significant structural moiety and functionalization of the C–H bond in indole-containing molecules expands their chemical space, and modifies their properties and/or activities. Indole prenyltransferases (IPTs) catalyze the direct regio
Autor:
James Z. Deng, Amy Calamari, Samuel L. Graham, Christopher S. Burgey, Eric L. Moore, Craig M. Potteiger, Jixin Wang, Carolyn Segerdell, Daniel V. Paone, James Mulhearn, Cuyue Tang, Diem N. Nguyen, Kerry L. Fillgrove, Shaun R. Stauffer, Michael D. Leitl, Annie Liang, Mark O. Urban, Anthony Ginnetti, Gong Cheng, Anthony W. Shaw, Stefanie A. Kane, Jacqueline Panigel, Christopher A. Salvatore, Sean P. Cook, Juliana Anquandah
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1392-1396
A second-generation small molecule P2X3 receptor antagonist has been developed. The lead optimization strategy to address shortcomings of the first-generation preclinical lead compound is described herein. These studies were directed towards the iden
Autor:
Anthony W. Shaw, Theresa M. Williams, Joseph P. Vacca, Scott D. Mosser, Sean Yu, Christopher A. Salvatore, Craig M. Potteiger, Stefanie A. Kane, Diem N. Nguyen, Christopher S. Burgey, James Z. Deng, Shane Roller, Daniel V. Paone, Harold G. Selnick
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2683-2686
In our ongoing efforts to develop CGRP receptor antagonists for the treatment of migraine, we aimed to improve upon telecagepant by targeting a compound with a lower projected clinical dose. Imidazoazepanes were identified as potent caprolactam repla
Autor:
Samuel L. Graham, James Z. Deng, Diem N. Nguyen, Victor K. Johnston, James C. Hershey, Bradley K. Wong, Christopher A. Salvatore, Cynthia Miller-Stein, Kenneth S. Koblan, Christopher S. Burgey, Scott D. Mosser, Daniel V. Paone, Stefanie A. Kane, Anthony W. Shaw, Theresa M. Williams, Joseph P. Vacca
Publikováno v:
Journal of Medicinal Chemistry. 50:5564-5567
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Herein we describe optimization of CGRP receptor antagonists based on an earlier lead structure containing a (3R)-amino-(6S)-phenylcaprolactam core. Replaceme
Autor:
Amy G. Quigley, Daniel V. Paone, Melody Mcwherter, Andrew Danziger, Brendan M. Crowley, Mark E. Fraley, Danny Gauvreau, Dan Cui, Karsten Menzel, J. Christopher Culberson, Joseph G. Bruno, Vijay Bhasker G. Reddy, Christopher A. Salvatore, Ian M. Bell, Craig A. Stump, Christopher S. Burgey, Eric L. Moore, Stefanie A. Kane, Amanda L. Kemmerer, Scott D. Mosser, Christine Fandozzi, Diem N. Nguyen, Craig M. Potteiger, Harold G. Selnick, Rebecca B. White
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(21)
In our efforts to develop CGRP receptor antagonists as backups to MK-3207, 2, we employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds. The development of a structurally diverse, potent (20, cAMP+HS IC50=0.6
Autor:
Beth R. Norton, Ruth Z. Rutledge, Amy G. Quigley, Diem N. Nguyen, Theresa M. Williams, Scott D. Mosser, Christopher S. Burgey, Joseph P. Vacca, James Z. Deng, Samuel L. Graham, Stefanie A. Kane, Ian M. Bell, Christopher A. Salvatore, Craig A. Stump, Kenneth S. Koblan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5052-5056
In our continuing effort to identify CGRP receptor antagonists for the acute treatment of migraine, we have undertaken a study to evaluate alternative 4-substituted piperidines to the lead dihydroquinazolinone 1. In this regard, we have identified th
Autor:
Diem N. Nguyen, Samuel L. Graham, Theresa M. Williams, Scott D. Mosser, Ian M. Bell, Bang-Lin Wan, Kimberly Della Penna, Priya Kunapuli, Stefanie A. Kane, Craig A. Stump, Ruth Z. Rutledge, John F. Fay, Ken S. Koblan, Joseph P. Vacca, C. Blair Zartman, Steven N. Gallicchio, Amy G. Quigley, Christopher A. Salvatore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2595-2598
High-throughput screening of the Merck sample collection identified benzodiazepinone tetralin-spirohydantoin 1 as a CGRP receptor antagonist with micromolar activity. Comparing the structure of 1 with those of earlier peptide-based antagonists such a
Autor:
Diem N. Nguyen, Mary Beth O'Connell
Publikováno v:
Pharmacotherapy. 22:1047-1054
Study Objective. To quantify Asian and Asian-American college students' knowledge of osteoporosis and preventive health behaviors. Design. Sixty-four-question survey. Setting. University of Minnesota. Subjects. One hundred sixty-eight male and female
Autor:
Carolyn A. Buser, Christine Fernandes, Diem N. Nguyen, Michelle Ellis-Hutchings, Robert B. Lobell, Ronald G. Robinson, Craig A. Stump, Hans E. Huber, Eileen S. Walsh, Theresa M. Williams, Joseph P. Davide
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1269-1273
Compound 1 has been shown to be a dual prenylation inhibitor with FPTase (IC50=2 nM) and GGPTase-I (IC50=95 nM). Analogues of 1, which replaced the cyanophenyl group with various biaryls, led to the discovery of highly potent dual FPTase/GGPTase-I in
Autor:
Diem N. Nguyen, et al. et al.
Publikováno v:
ChemInform. 33