Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Eric C. Bigham"'
Autor:
Stephen C. McKeown, Thomas R. Littleton, Andrew J. Peat, Steve P. Watson, Aaron S. Goetz, Deirdre Mary Bernadette Hickey, David F. Corbett, Celia P. Briscoe, Eric C. Bigham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1584-1589
The discovery, synthesis and structure-activity relationship (SAR) of novel carboxylic acid agonists for GPR40 are described. Aryl propionic acid 1, identified from a high throughput screen, was selected for chemical exploration. Compound 2 was ident
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1710461fe4ffcfb7fb679fdb991df2ad
https://doi.org/10.1016/j.bmcl.2006.12.084
https://doi.org/10.1016/j.bmcl.2006.12.084
Autor:
Francis X. Tavares, Paul L. Feldman, Ronda J. Ott, Kamal A. Al-Barazanji, Huiqiang Zhou, Yu C. Guo, David L. Carlton, Daniel G. Lang, Michael J. Bishop, and Andrew J. Peat, Donald L. Hertzog, Mary K. Grizzle, Aaron S. Goetz, Anthony L. Handlon, Christy S. Britt, Eric C. Bigham, Diane M. Ignar
Publikováno v:
Journal of Medicinal Chemistry. 49:7095-7107
The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat diet-induced obesity of MCH KO mice has spurred considerable efforts to develop small molecule
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba88ed96984bac23ce99ed146435ec5d
https://doi.org/10.1021/jm060572f
https://doi.org/10.1021/jm060572f
Autor:
Bryan W. Sherman, Jason D. Speake, M. Jeffrey Gobel, Deanna T. Garrison, Eric C. Bigham, Frank Navas, Paul E. Irving, David L. Saussy, James A Liacos, Michael J. Bishop, Stephen J. Hodson
Publikováno v:
Journal of Medicinal Chemistry. 45:2229-2239
A series of 2'-alkylthio-2-(anilinomethyl)imidazolines were prepared to examine the effect of the alkyl group size, sulfur oxidation state, and phenyl ring substitution on ligand binding and agonism of alpha-adrenergic receptor subtypes alpha1a, alph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61ef6b80bbfca9f23207336a1dc43a40
https://doi.org/10.1021/jm000542r
https://doi.org/10.1021/jm000542r
Autor:
Craig S. Regitz, Eric E. Boros, Vicente Samano, John A. Ray, Paul L. Feldman, Cecilia S. Koble, Michael Tolar Martin, James B. Thompson, David Kendall Jung, Eric C. Bigham, Robert A. Mook
Publikováno v:
Organic Letters. 1:1993-1996
[formula: see text] The stereo- and regioselective synthesis of ultra-short-acting nondepolarizing neuromuscular blocker GW 0430 (5a) is described. Key steps involved the enantioselective transfer hydrogenation of imine 8 employing Noyori's catalyst,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cdb86af889e9e4887429827930208603
https://doi.org/10.1021/ol9911573
https://doi.org/10.1021/ol9911573
Publikováno v:
ChemInform. 25
Analogues of N-[4-[[3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl]amino] benzoyl]-L-glutamic acid (5-DACTHF), in which the phenylene group is replaced by either a thienoyl or a thiazolyl group were synthesized. These compounds were prepared b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::128b19aaa76430972e639863f5cae344
https://doi.org/10.1002/chin.199450218
https://doi.org/10.1002/chin.199450218
Autor:
Robert J. Mullin, S Singer, H. R. Wilson, Eric C. Bigham, Barry R. Keith, L S Heath, K A Waters, David S. Duch, R. Ferone
Publikováno v:
Biochemical Pharmacology. 43:1627-1634
This study compares the antitumor activity and metabolism of the purine de novo biosynthesis inhibitor 5-deazaacyclotetrahydrofolate and a series of analogues. All compounds have similar IC50 values for inhibition of MCF-7 cell growth, activity of gl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a8f32a233696851e6803a8c3add811a
https://doi.org/10.1016/0006-2952(92)90222-5
https://doi.org/10.1016/0006-2952(92)90222-5
Publikováno v:
Journal of Biological Chemistry. 267:5599-5607
N-Acetylserotonin (compound 1) and N-acetyldopamine (compound 7) inhibit bovine adrenal medullary sepiapterin reductase in a manner competitive with the pterin substrate and have Ki values of 0.12 and 0.4 microM, respectively. Molecular modeling sugg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::078b7e033bc13c753109822be4792cd3
https://doi.org/10.1016/s0021-9258(18)42807-4
https://doi.org/10.1016/s0021-9258(18)42807-4
Autor:
Diane M. Ignar, Dulce Garrido, Francis X. Tavares, Yu C. Guo, Huiqiang Zhou, Kamal A. Al-Barazanji, David L. Carlton, Joel P. Cooper, Donald L. Hertzog, Andrew J. Peat, Aaron S. Goetz, Michael J. Bishop, Alex J. Daniels, Ronda O. Morgan, Anthony L. Handlon, Christy S. Britt, Eric C. Bigham, Mary K. Grizzle
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(18)
Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e402dd391f79c0bb828840ed2301097e
https://pubmed.ncbi.nlm.nih.gov/16870432
https://pubmed.ncbi.nlm.nih.gov/16870432
Autor:
John S. Walsh, Mir Hashim, Michael Tolar Martin, David Kendall Jung, Gary D. Bowers, Virgil L. Styles, Istvan Kaldor, Caroline L. Moseley, John A. Ray, Vicente Samano, Randy D. Rutkowske, Cecilia S. Koble, Timothy D. Spitzer, Patel Sanjay Shashikant, Eric E. Boros, Andrea M. Sefler, G. Evan Boswell, James C. Wisowaty, Matthew R. Belmont, Mindy J. Reese, Paul L. Feldman, James B. Thompson, Robert A. Mook, Eric C. Bigham, John J. Savarese
Publikováno v:
Journal of medicinal chemistry. 46(12)
Structure-activity relationships in rhesus monkeys for a novel mixed-onium class of ultra-short-acting nondepolarizing tetrahydroisoquinolinium neuromuscular blockers (NMBs) are described. Bis-onium chlorofumarate 20a with (1R,2S)-benzyltetrahydroiso
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4a53d6f4ad55fda401dbe78fe5f016b
https://pubmed.ncbi.nlm.nih.gov/12773054
https://pubmed.ncbi.nlm.nih.gov/12773054
Autor:
Stephen J. Hodson, Jason D. Speake, Bryan W. Sherman, David L. Saussy, Michael J. Bishop, Eric C. Bigham, Frank Navas, Deanna T. Garrison, Jim A. Liacos, Paul E. Irving
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(6)
The structure-activity relationship of 2'-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as alpha(1) adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ee58155b3bd80c7824bcef033ead499
https://pubmed.ncbi.nlm.nih.gov/12643939
https://pubmed.ncbi.nlm.nih.gov/12643939