Zobrazeno 1 - 10
of 27
pro vyhledávání: '"William G. Earley"'
Autor:
Zheng Tan, Steve Sorota, Deen Tulshian, R. Jason Herr, William G. Earley, Charles R. Heap, Stephanie Brumfield, Terry Bridal, Jennifer Hanisak, Xiaoping Zhou, Julius Matasi, Ana Bercovici, Ginny D. Ho, Diane Rindgen, Brandy Courneya, Shu-Wei Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4110-4113
A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these anal
Publikováno v:
Tetrahedron Letters. 50:3813-3816
A highly efficient one-pot, three-component microwave-assisted procedure has been developed for the preparation of 1-(para-substituted-aryl)-4-(2-acetoxyethyl)piperazines and 1-(para-substituted-aryl)-4-(2-acetoxyethyl)piperidines. Microwave-accelera
Publikováno v:
Journal of Combinatorial Chemistry. 11:355-363
A highly efficient procedure was developed for the microwave-assisted synthesis of N-heteroaryl-4-(2-chloroethyl)piperazines and N-heteroaryl-4-(2-chloroethyl)piperidines. Microwave irradiation of electron deficient heteroaryl chlorides with 1,4-diaz
Autor:
Dana A. Razzano, John F. Quinn, Brian T. Gregg, William G. Earley, W. Martin Rennells, Kathryn C. Golden, Jennifer L. Butcher, Dacia A. Maynard, Dmytro O. Tymoshenko
Publikováno v:
Journal of Combinatorial Chemistry. 9:1036-1040
An efficient and rapid solution phase combinatorial synthesis of a 3-substituted 5-arylidene-1-methyl-2-thiohydantoin library was developed. The salient feature for this library production procedure is the addition of the Lewis acid catalyst, indium(
Autor:
Robert Lewis, David J. Fairfax, David M. Jenkins, Andrew J. Zych, Hong-Jun Wang, Rajiv R. Srivastava, William G. Earley
Publikováno v:
Tetrahedron Letters. 48:3043-3046
A highly efficient one-pot, two-step microwave procedure has been developed for the synthesis of 4-substituted 1-heteroarylpiperazines. Microwave heating of heteroaryl chlorides with 1,4-diazabicyclo[2.2.2]octane (DABCO) at 160 °C for 15 min yielded
Autor:
W. Martin Rennells, Dana A. Razzano, Kathryn C. Golden, William G. Earley, Brian T. Gregg, John F. Quinn
Publikováno v:
Synthesis. 2006:4200-4204
A survey of Lewis acids was conducted to facilitate the formation of arylidenethiohydantoins. The use of indium(III) triflate shows significant advantages in facilitating this reaction. In most examples, the Lewis acid promoted catalysis gave shorter
Autor:
G. Patrick Meier, William G. Earley, Matthew J. Sharp, Taeboem Oh, Andrew Madin, Jon E. Jacobsen, Larry E. Overman, Christopher J. O’Donnell, David W. Old
Publikováno v:
Journal of the American Chemical Society. 127:18046-18053
A detailed examination of the use of aza-Cope rearrangement-Mannich cyclization sequences for assembling the azatricyclo[4.4.0.0(2,8)]decane core of gelsemine is described. Iminium ions and N-acyloxyiminium ions derived from endo-oriented 1-methoxy-
Autor:
Cheng Guo, Liaqat Masih, David D. Manning, Peter R. Guzzo, Kristen N. Ryan, Jonathan D. Wierschke, Sok Hui Choo, William G. Earley, Nicholas M. Barnes, Zhenjun Zhang, Jennifer Naginskaya, Amy S Newman, Catherine A. Brady
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(11)
Serotonin type 3 (5-HT3) receptor partial agonists have been targeted as potential new drugs for the symptomatic relief of irritable bowel syndrome (IBS). Multiple diazepinone-based compounds have been discovered, which exhibit nanomolar binding affi
Autor:
Michael D. Kelly, Brian Ault, Virendra Kumar, Lisa D. Aimone, William G. Earley, John P. Mallamo, Diane L. DeHaven-Hudkins, John A. Dority, Chakrapani Subramanyam, Matthew S. Miller
Publikováno v:
Journal of Medicinal Chemistry. 38:3586-3592
A series of permanently charged benzo[b]quinolizinium cations having lower lipophilicity than MK-801 or phencyclidine (PCP) were synthesized. Data relating agonist independent block of N-methyl-D-aspartic acid (NMDA) ion channels to log D are describ
Autor:
Chakrapani Subramanyam, William G. Earley, Joseph R. Wetzel, John P. Mallamo, Diane L. DeHaven-Hudkins, Gary M. Pilling, Philip M. Carabateas, Timothy Allen, Rudolph K. Kullnig
Publikováno v:
Journal of Medicinal Chemistry. 38:2483-2489
The synthesis and in vitro and in vivo evaluation of 12,13-cycloalkyl-6,11-ethanobenzo[b]-quinolizidines, a new class of noncompetitive N-methyl-D-aspartate (NMDA) antagonists acting at the PCP site on the NMDA receptor complex, is reported. Structur