Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Rajagopal Bakthavatchalam"'
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:
Yu-Wen Li, Xiao-Xin Yan, Robert Zaczek, Shimoga R. Prakash, Ning Huang, David H. Rominger, Rajagopal Bakthavatchalam, Paul J. Gilligan, Anne Marshall, Xiaoping Qi, Ge Zhang, Cynthia M. Rominger, Geraldine Hill
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 305:57-69
The in vitro pharmacological profile of a novel small molecule corticotropin-releasing factor 1 (CRF1) receptor antagonist, (±) -N -[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl)propyl)-6-methyl-1 H -1,2,3-triazolo[4,5- c ]pyridin-4-amine (SN003),
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0750fd315c2cc991680a214de8ad80ca
https://doi.org/10.1124/jpet.102.046128
https://doi.org/10.1124/jpet.102.046128
Publikováno v:
Expert opinion on therapeutic patents. 24(7)
Leucine-rich repeat kinase 2 (LRRK2) is a large (2527 residues) complex multi-domain protein that has GTPase and kinase domains. Autosomal dominant missense mutations in LRRK2 have been found in individuals with Parkinson's disease (PD) and are consi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03d17bbd01b8dbded4f0236690f5c559
https://pubmed.ncbi.nlm.nih.gov/24918198
https://pubmed.ncbi.nlm.nih.gov/24918198
Autor:
Argyrios G. Arvanitis, Paul J. Gilligan, Robert J. Chorvat, Robert S. Cheeseman, Thomas E. Christos, Rajagopal Bakthavatchalam, James P. Beck, Anthony J. Cocuzza, Frank W. Hobbs, Richard G. Wilde, Charles Arnold, Dennis Chidester, Matthew Curry, Liqi He, Andrea Hollis, John Klaczkiewicz, Paul J. Krenitsky, Joseph P. Rescinito, Everett Scholfield, Steven Culp, Errol B. De Souza, Lawrence Fitzgerald, Dimitri Grigoriadis, S. William Tam, Y. Nancy Wong, Shiew-Mei Huang, Helen L. Shen
Publikováno v:
Journal of Medicinal Chemistry. 42:805-818
Screening of our chemical library using a rat corticotropin-releasing hormone (CRH) receptor assay led to the discovery that 2-anilinopyrimidine 15-1 weakly displaced [125I]-0-Tyr-oCRH from rat frontal cortex homogenates when compared to the known pe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f81d62a04a50c26bdbe0a34ca2ad02c
https://doi.org/10.1021/jm980222w
https://doi.org/10.1021/jm980222w
Publikováno v:
Journal of Heterocyclic Chemistry. 33:213-216
Treatment of benzaldehyde l-(2-propenyl)-4-methylsulfonylphenylhydrazone (1f) with 45% sulfuric acid gave 2-(4-methylsulfonylphenyl)-6-phenylhexahydro-4-pyridazinol (2f) in 35% yield rather than the expected 1-(4-methylsulfonylphenyl)-1-(2-propenyl)h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2e60100de7310d538ff7c2a5aba23fcf
https://doi.org/10.1002/jhet.5570330137
https://doi.org/10.1002/jhet.5570330137
Publikováno v:
ChemInform. 27
Treatment of benzaldehyde l-(2-propenyl)-4-methylsulfonylphenylhydrazone (1f) with 45% sulfuric acid gave 2-(4-methylsulfonylphenyl)-6-phenylhexahydro-4-pyridazinol (2f) in 35% yield rather than the expected 1-(4-methylsulfonylphenyl)-1-(2-propenyl)h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::13e237ae3b8b86a81a2d980940872f66
https://doi.org/10.1002/chin.199630190
https://doi.org/10.1002/chin.199630190
Autor:
Scott M. Capitosti, Bertrand L. Chenard, Beth Ann Murphy, Xiaozhang Zheng, A. Brian Jones, Kevin J. Hodgetts, Susan Boyce, Daniel N. Cortright, Charles A. Blum, Rajagopal Bakthavatchalam, James E. Krause, Timothy M. Caldwell, Marci Crandall
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(15)
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a non-selective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2645ca5f19d330c33fc4f42e30cf2a46
https://pubmed.ncbi.nlm.nih.gov/20615696
https://pubmed.ncbi.nlm.nih.gov/20615696
Publikováno v:
Current topics in medicinal chemistry. 11(17)
TRPA1 is a member of a superfamily of non-selective cation channels that is known to be involved in multiple physiological functions. TRPA1 is activated by a broad spectrum of chemical irritants and endogenous inflammatory compounds. An emerging role
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50826232acba353e6690cc01f2ddd543
https://pubmed.ncbi.nlm.nih.gov/21671872
https://pubmed.ncbi.nlm.nih.gov/21671872