Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Gregory A, Gfesser"'
Autor:
Marc J C, Scanio, Xenia B, Searle, Bo, Liu, John R, Koenig, Robert J, Altenbach, Gregory A, Gfesser, Andrew, Bogdan, Stephen, Greszler, Gang, Zhao, Ashvani, Singh, Yihong, Fan, Andrew M, Swensen, Timothy, Vortherms, Arlene, Manelli, Corina, Balut, Wenqing, Gao, Hong, Yong, Michael, Schrimpf, Chris, Tse, Philip, Kym, Xueqing, Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 72:128843
Cystic fibrosis (CF) is an autosomal recessive disease resulting from mutations on both copies of the CFTR gene. Phenylalanine deletion at position 508 of the CFTR protein (F508del-CFTR) is the most frequent mutation in CF patients. Currently, the mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15a2a884faa7901f5e486831d30b03cd
https://doi.org/10.1016/j.bmcl.2022.128843
https://doi.org/10.1016/j.bmcl.2022.128843
Autor:
Wenqing Gao, Robert J. Altenbach, Gang Zhao, John R. Koenig, Greszler Stephen N, Searle Xenia B, Gregory A. Gfesser, Hong Yong, Corina Balut, Marc J. C. Scanio, Yihong Fan, Michael R. Schrimpf, Philip R. Kym, Timothy A. Vortherms, Andrew M. Swensen, Bo Liu, Arlene M. Manelli, Ying Jia, Xueqing Wang, Chris Tse, Andrew Bogdan, Ashvani K. Singh
Publikováno v:
ACS Med Chem Lett
[Image: see text] Cystic fibrosis (CF) is a genetic disorder that affects multiple tissues and organs. CF is caused by mutations in the CFTR gene, resulting in insufficient or impaired cystic fibrosis transmembrane conductance regulator (CFTR) protei
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::418648a24d9417696c73d206f53310b2
https://doi.org/10.1021/acsmedchemlett.9b00377
https://doi.org/10.1021/acsmedchemlett.9b00377
Autor:
Philip R. Kym, Arthur Gomtsyan, Gregory A. Gfesser, Bin Li, Regina M. Reilly, Bruce Clapham, Jerome F. Daanen, Rodger F. Henry, Torben R. Neelands, Pamela S. Puttfarcken, Susan M. Huang, Robert G. Schmidt, Robert J. Altenbach, S.K. Joshi, Huaqing Liu, Marlon D. Cowart, David N. Whittern, Phil B. Cox, Jill-Desiree Brederson, Michael J. Dart, Anurupa Shrestha, Donna Gauvin, Michael E. Kort, Erol K. Bayburt, Ping Song, Steve McGaraughty, Connie R. Faltynek, Heath A. McDonald, Patricia N. Banfor, Diana Schmidt, Eric A. Voight, Mohamad Shebley, Jason A. Segreti
Publikováno v:
Journal of Medicinal Chemistry. 59:4926-4947
Transient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd1b773984159dd5e2a719a0398228e6
https://doi.org/10.1021/acs.jmedchem.6b00287
https://doi.org/10.1021/acs.jmedchem.6b00287
Autor:
Kathy Sarris, Clark A. Briggs, Gregory A. Gfesser, William H. Bunnelle, Sujatha M. Gopalakrishnan, Michael P. Curtis, Caroline Wetterstrand, Ramin Faghih, Richard J. Radek, John Malysz, Holly M. Robb, Jens Halvard Grønlien, Hilde Ween, Kennan C. Marsh, Rachid El-Kouhen, Murali Gopalakrishnan
Publikováno v:
Journal of Medicinal Chemistry. 52:3377-3384
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of alpha7 nAChRs is described. Optimization of this series led to the identification of 19 (A-867744), a novel type II PAM with good potency and selectivity. Co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d26e322c761752b465f16f2e130987ba
https://doi.org/10.1021/jm9003818
https://doi.org/10.1021/jm9003818
Autor:
Ivan Milicic, Jorge D. Brioni, Deliang Zhou, Gerard B. Fox, Gerard D. Gagne, Ramin Faghih, Angela L. Molesky, Arthur A. Hancock, Kennan C. Marsh, Liping Pan, David G. Witte, Timothy A. Esbenshade, Jill M. Wetter, Kaitlin E. Browman, Michael J. Buckley, Gilbert Diaz, Xiaoqing Deng, Victoria A. Komater, John L. Baranowski, Thomas R. Miller, Marlon D. Cowart, Gregory A. Gfesser, Marilyn S. Diehl, Kathleen M. Krueger, Ellen M. Roberts
Publikováno v:
Biochemical Pharmacology. 73:1243-1255
Three novel heterocyclic benzofurans A-688057 ( 1 ), A-687136 ( 2 ), and A-698418 ( 3 ) were profiled for their in vitro and in vivo properties as a new series of histamine H 3 receptor antagonists. The compounds were all found to have nanomolar pote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fc1120f3945a2a50635d43ffdb23648
https://doi.org/10.1016/j.bcp.2007.02.010
https://doi.org/10.1016/j.bcp.2007.02.010
Autor:
Meiqun Jiang, Stanley Didomenico, Ronald D. Snyder, Karen M. Alexander, Shripad S. Bhagwat, Guo Zhu Zheng, Carol T. Wismer, Haixia Yu, Andrew O. Stewart, Marilyn S. Diehl, Gregory A. Gfesser, Kennan C. Marsh, Erol K. Bayburt, Robin R. Frey, Mark A. Matulenko, Marlon D. Cowart, Jeffery A. McKie, Arthur Gomtsyan, Kathy L. Kohlhaas, Michael F. Jarvis, Elizabeth A. Kowaluk, Joseph P. Mikusa, Steve McGaraughty, Chih-Hung Lee
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:3705-3720
4-Amino-5,7-disubstituted pyridopyrimidines are potent, non-nucleoside inhibitors of adenosine kinase (AK). We recently identified a potent, orally efficacious analog, 4 containing a 7-pyridylmorpholine substituted ring system as the key structural e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f95502834c737e63cdbb31651581d988
https://doi.org/10.1016/j.bmc.2005.03.023
https://doi.org/10.1016/j.bmc.2005.03.023
Autor:
Betty B. Yao, Ramin Faghih, Thomas R. Miller, Henry Zhang, Youssef L. Bennani, Timothy A. Esbenshade, David G. Witte, Gregory A. Gfesser, Gerard B. Fox, Jia Bao Pan, Arthur A. Hancock, Chae-Hee Kang, Jürgen Dinges, Kathy M. Krueger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:673-676
Further SAR studies on novel histamine H(3) receptor antagonists are presented. Compound 14bb is a potent antagonist of both the rat cortical and human clone receptors, and is demonstrated to act functionally as an antagonist in an in vivo mouse dips
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fed226c898efdb95d448246274d9c2d1
https://doi.org/10.1016/j.bmcl.2003.11.038
https://doi.org/10.1016/j.bmcl.2003.11.038
Autor:
Haixia Yu, Michael F. Jarvis, Gregory A. Gfesser, Marlon D. Cowart, Elizabeth A. Kowaluk, Karen M. Alexander, John R. Koenig, Chang Zhu, Joseph P. Mikusa, Andrew O. Stewart, John K. Pratt, Chih-Hung Lee, Guo Zhu Zheng, Carol T. Wismer, Kathy L. Kohlhaas, Richard J. Perner, Yue Mao, Steve McGaraughty, Katharine L. Chu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3041-3044
We have discovered that polar 7-substituents of pyridopyrimidine derivatives affect not only whole cell AK inhibitory potency, but also selectivity in causing locomotor side effects in vivo animal models. We have identified compound, 1o, which has po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4c93f31bd4e5393026e8ea8be633d95
https://doi.org/10.1016/s0960-894x(03)00642-5
https://doi.org/10.1016/s0960-894x(03)00642-5
Publikováno v:
Tetrahedron Letters. 35:1661-1664
Lewis acid-promoted reactions of unsymmetrically substituted (E)-stilbenes with 2-methoxy-1,4-benzoquinones regio- and stereoselectively produce trans 2,3-diaryl-2,3-dihydrobenzofurans.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::55ae60cf0a185b706f62271105b89bc1
https://doi.org/10.1016/0040-4039(94)88313-0
https://doi.org/10.1016/0040-4039(94)88313-0
Publikováno v:
ChemInform. 39
During the preparation of 6-bromoisoquinolinone, a novel and unexpected reaction occurred to form a pyridinone and a pyrimidine-2,4-dione. We propose a [4+2] Diels-Alder dimerization of an intermediate styrene-isocyanate to explain the observed produ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1a201aba4dbab488fb1fc9e34e2468c5
https://doi.org/10.1002/chin.200839033
https://doi.org/10.1002/chin.200839033