Zobrazeno 1 - 10
of 76
pro vyhledávání: '"John E. Starrett"'
Autor:
Vincenzo Calandra, Steven I. Dworetzky, Yong-Jin Wu, Ronald J. Knox, William Fitzpatrick, Huan He, JoAnne E Natale, David G. Harden, Li-Qiang Sun, Carl D. Davis, David Weaver, Frederic Machet, Joseph Polino, John E. Starrett, Karen Heman, Ping Chen, Valentin K. Gribkoff, Christopher G. Boissard, Clotilde Bourin, Charles M. Conway, Jie Chen, Mark W. Thompson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6188-6191
Acrylamide (S)-6, a potent and efficacious KCNQ2 (Kv7.2) opener, demonstrated significant activity in two models of neuropathic pain and in the formalin test, suggesting that KCNQ2 openers may be useful in the treatment of neuropathic pain including
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c81071ad17f712c14b9149ad6dfe150
https://doi.org/10.1016/j.bmcl.2013.08.092
https://doi.org/10.1016/j.bmcl.2013.08.092
Autor:
JoAnne E Natale, Jeffrey L. Romine, Valentin K. Gribkoff, Astrid A. Ortiz, Qi Gao, Christopher G. Boissard, Lorraine Pajor, Scott W. Martin, Sandra L. Moon, Swamy Yeleswaram, John E. Starrett, Steven I. Dworetzky, Nicholas A. Meanwell
Publikováno v:
Journal of Medicinal Chemistry. 50:528-542
Compound 8a (BMS-191011), an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel ope
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65a54fd4d8be30acec58a394f052e212
https://doi.org/10.1021/jm061006n
https://doi.org/10.1021/jm061006n
Autor:
Alain Martel, Li-Qiang Sun, Jie Chen, Huan He, Ronald J. Knox, David G. Harden, JoAnne E Natale, Steven I. Dworetzky, Yong-Jin Wu, Alexandre L'Heureux, David Weaver, John E. Starrett, Mark W. Thompson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:363-366
Replacement of the morpholinyl moiety in (S,E)-N-[1-(3-morpholinophenyl)ethyl]-3-phenylacrylamide (1) with heteroaryl groups led to the identification of (S,E)-N-1-[3-(6-fluoropyridin-3-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (5) as a potent KCN
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb33adb537a4bf34b46494a7e279e57f
https://doi.org/10.1016/j.bmcl.2004.10.065
https://doi.org/10.1016/j.bmcl.2004.10.065
Autor:
Jean-Paul Daris, John E. Starrett, Pierre Dextraze, Rick L. Pieschl, Huan He, David G. Harden, David Weaver, Jie Chen, Yong-Jin Wu, Ronald J. Knox, Valentin K. Gribkoff, Li-Qiang Sun, Qi Gao, Mark W. Thompson, Dedong Wu, Christopher G. Boissard, Steven I. Dworetzky, William Fitzpatrick, JoAnne E Natale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4533-4537
Bioisosteric replacement studies led to the identification of N -(1-benzo[1,3]dioxol-5-yl-ethyl)-3-(2-chloro-phenyl)-acrylamide (( S )- 3 ) as a highly potent KCNQ2 opener, and 3-(2,6-difluoro-phenyl)- N -[1-(2,3-dihydro-benzofuran-5-yl)-ethyl]-acryl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca337a8d17cff2971f2f629786972798
https://doi.org/10.1016/j.bmcl.2004.06.035
https://doi.org/10.1016/j.bmcl.2004.06.035
Autor:
Li-Qiang Sun, John E. Starrett, Pierre Dextraze, Steven I. Dworetzky, Jie Chen, Valentin K. Gribkoff, JoAnne E Natale, Alexandre L'Heureux, Huan He, Yong-Jin Wu, Christopher G. Boissard
Publikováno v:
Journal of Medicinal Chemistry. 47:2887-2896
A new class of acrylamides was synthesized, and the effects of these analogues on outward potassium current were evaluated by using two electrode voltage clamp recordings from Xenopus laevis oocytes expressing cloned mKCNQ2 channels. SAR studies indi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5d840cd436522d126aee225be30809c
https://doi.org/10.1021/jm0305826
https://doi.org/10.1021/jm0305826
Autor:
Joanne T. Natale, John E. Starrett, Piyasena Hewawasam, Valentin K. Gribkoff, Min Ding, Christopher G. Boissard, Sarita W Yeola, Nathan Chen, Steven I. Dworetzky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1615-1618
3-Amino-4-benzylquinolin-2-ones have been identified as a novel class of KCNQ2 channel openers. Synthesis and SAR is described along with their electrophysiological evaluation as activators of the cloned m KCNQ2 channel expressed in Xenopus laevis oo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4947a4b4aad6acaab3b34b31f5971cf5
https://doi.org/10.1016/j.bmcl.2004.01.073
https://doi.org/10.1016/j.bmcl.2004.01.073
Autor:
Christopher G. Boissard, Huan He, David Weaver, Valentin K. Gribkoff, David G. Harden, Jie Chen, Qi Gao, Mark W. Thompson, Li-Qiang Sun, Dedong Wu, William Fitzpatrick, JoAnne E Natale, John E. Starrett, Yong-Jin Wu, Rick L. Pieschl, Ronald J. Knox, Steven I. Dworetzky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1991-1995
(S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-2) was identified as a potent and efficacious KCNQ2 opener. This compound demonstrated significant activity in reducing neuronal hyperexcit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::73ffe93db9f647df1e793f8446a06bbc
https://doi.org/10.1016/j.bmcl.2004.01.069
https://doi.org/10.1016/j.bmcl.2004.01.069
Autor:
Shing Hong Kang, Svetlana Tertyshnikova, Michael Sinz, Sanna Lehtinen-Oboma, John E. Starrett, Yong-Jin Wu, Steven I. Dworetzky, Alexandre L'Heureux, Digavalli V. Sivarao, Mark W. Thompson, Gene G. Kinney, Christopher G. Boissard, Amy Newton, David Weaver, Henry S. Wong, Ronald J. Knox, Valentin K. Gribkoff, Li-Qiang Sun, Lei Zhang, JoAnne E Natale, Corinne R. Greco, Huan He, David G. Harden
Publikováno v:
Journal of Medicinal Chemistry. 46:3197-3200
(S)-N-[1-(3-Morpholin-4-ylphenyl)ethyl]-3-phenylacrylamide (2) was synthesized as an orally bioavailable KCNQ2 potassium channel opener. In a rat model of migraine, 2 demonstrated significant oral activity in reducing the total number of cortical spr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::071a82a89a8a915e31f48b6c58bd4901
https://doi.org/10.1021/jm034073f
https://doi.org/10.1021/jm034073f
Autor:
John E. Starrett, Piyasena Hewawasam, Douglas D. Dischino, J. Kent Rinehart, Valentin K. Gribkoff, George M. Luke, Tony L. Spears
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 46:139-149
The syntheses of tritium labeled (S)-3-(5-chloro-2-[OC3H3]methoxyphenyl-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one, and carbon-14 (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-[2,3-14C2] indol-2-one are rep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::44dc4d4b571e20c082aebcedb326b030
https://doi.org/10.1002/jlcr.652
https://doi.org/10.1002/jlcr.652
Autor:
Lawrence R. Marcin, James J. Mongillo, Douglas D. Dischino, Edward S. Kozlowski, Kevin W. Gillman, John E. Starrett, Heidi Dulac, Lynn S. Keller
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 46:1161-1171
The syntheses of (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-[18F]-fluoro-6-(trifluoromethyl)-1H-indol-2-one was accomplished by the microwave assisted carrier-added 18F fluorination of (R,S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-chloro-6-(tr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::563360732071e98549164723d0e5da80
https://doi.org/10.1002/jlcr.748
https://doi.org/10.1002/jlcr.748