Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Harry Brielmann"'
Autor:
Harry Brielmann, David J. Matson, Bertrand L. Chenard, Mark T. Kershaw, W. Rycroft, Nicola Burnaby-Davies, Marci Crandall, Stéphane De Lombaert, Kevin J. Hodgetts, William J. Martin, Rajagopal Bakthavatchalam, Beth Ann Murphy, Timothy M. Caldwell, G Mason, A. Brian Jones, Xiaozhang Zheng, Helen Perrett, Susan Boyce, James E. Krause, Daniel N. Cortright, Charles A. Blum, Rachael Conley, Scott M. Capitosti
Publikováno v:
Journal of Medicinal Chemistry. 53:3330-3348
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8f2448f051999a0038881eaa30e2452
https://doi.org/10.1021/jm100051g
https://doi.org/10.1021/jm100051g
Autor:
Rajagopal Bakthavatchalam, Lawrence K. Fung, Bertrand L. Chenard, David J. Matson, Chu K. Ngo, Marci Crandall, Stéphane De Lombaert, Daniel N. Cortright, Harry Brielmann, Charles A. Blum, Mark T. Kershaw, Jayaraman Chandrasekhar, Marta Day, Xiaozhang Zheng, James E. Krause, Kevin J. Hodgetts
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4573-4577
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b27714146b399be27941a08e67faa5fd
https://doi.org/10.1016/j.bmcl.2008.07.036
https://doi.org/10.1016/j.bmcl.2008.07.036
Autor:
Frank Burkamp, Kevin J. Hodgetts, Rajagopal Bakthavatchalam, Robert Clarkson, Hutchison Alan J, Stéphane De Lombaert, Daniel N. Cortright, A. Brian Jones, Charles A. Blum, Peter Blurton, Harry Brielmann, Xiaozhang Zheng, Jayaraman Chandrasekhar, Marci Crandall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5217-5221
Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. The development of B-ring SAR led to the conformationally constrained analog 70. The resulting aminoquinazoline 70 represents a novel VR1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6bfc1872ffb6d5bc79dc219aaca6d3f4
https://doi.org/10.1016/j.bmcl.2006.07.010
https://doi.org/10.1016/j.bmcl.2006.07.010
Autor:
Harry Brielmann
Publikováno v:
Natural Products from Plants ISBN: 9780849331343
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0df8ae72aa603338a8081096c08330d5
https://doi.org/10.1201/9781420049350.ch1
https://doi.org/10.1201/9781420049350.ch1
Publikováno v:
The Journal of Organic Chemistry. 49:1091-1095
On prepare les dihydro-1,2 dihydroxy-1,2benzo [b] fluoranthene et dihydro-11,12 dihydroxy-11,12 benzo [b] fluoranthene. L'activite mutagene vis-a-vis de Salmonella typhimurium T100 est moins grande que celle du benzo [b] fluoranthene
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::03764f70b05ec20f6526141e4fe9f11f
https://doi.org/10.1021/jo00180a026
https://doi.org/10.1021/jo00180a026