Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Alice Lee-Dutra"'
Autor:
Virginia M. Tanis, Dan Pippel, Cheryl A. Grice, Shelby Crawford, Jason P. Riley, Navin Rao, Karlsson Lars, Brad M. Savall, Christa C. Chrovian, Aimee Rose de Leon, Xiaohua Xue, Alejandro Santillan, Anne M. Fourie, Jimmy T. Liang, Xiaohu Deng, Jonathan M. Blevitt, Aaron M. Kearney, Arlene L. Young, Alice Lee-Dutra, Krystal Herman, Wendy Eccles, Rosa Luna, Jamila N. Booker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:811-815
Leukotrienes (LT's) are known to play a physiological role in inflammatory immune response. Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4). LTB(4) is a known pro-infl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c7e1edc94e27be30035be373870b432
https://doi.org/10.1016/j.bmcl.2012.11.074
https://doi.org/10.1016/j.bmcl.2012.11.074
Autor:
Jonathan M. Blevitt, Arlene L. Young, Xiaohua Xue, Genesis M. Bacani, Aimee Rose de Leon, Alejandro Santillan, Adrienne M. Landry-Bayle, Aaron M. Kearney, John J. M. Wiener, Laurent Gomez, Anne M. Fourie, Jason P. Riley, Krystal Herman, Christa C. Chrovian, Cheryl A. Grice, Shelby Crawford, Jay Nelson, Alice Lee-Dutra, Virginia M. Tanis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7504-7511
Previously, benzthiazole containing LTA4H inhibitors were discovered that were potent (1–3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering c Log D)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::35a5468ed5af090759b0400d5ef00168
https://doi.org/10.1016/j.bmcl.2012.10.036
https://doi.org/10.1016/j.bmcl.2012.10.036
Autor:
Brett D. Allison, Alice Lee-Dutra, Jamin D. Boggs, Brian Lord, Alejandro Santillan, Anita M. Everson, Kelly J. McClure, Timothy W. Lovenberg, Kirsten L. Morton, Cheryl A. Grice, Michael A. Letavic, Diane Nepomuceno, Nicholas I. Carruthers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6226-6230
Previous research on histamine H(3) antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two alkylamine groups. Recent investigation of the replacement of the central phenyl core with heteroar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef1b948e9b1e0331b19453a6508ea02f
https://doi.org/10.1016/j.bmcl.2010.08.103
https://doi.org/10.1016/j.bmcl.2010.08.103
Autor:
Lars Karlsson, Neelakandha S. Mani, Todd K. Jones, Steven Nguyen, Pragnya J. Desai, Cheryl A. Grice, Kristen L. Arienti, Robin L. Thurmond, Frank U. Axe, James P. Edwards, Mike Randal, Siquan Sun, Danielle K. Wiener, Michael K. Ameriks, Jing Liu, Alice Lee-Dutra, Damara Gebauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2370-2374
A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety may bind to the S3 pocket of the enzyme. Additional optimization led to the discovery of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c34a29a046072b572140132f3755f69
https://doi.org/10.1016/j.bmcl.2010.01.108
https://doi.org/10.1016/j.bmcl.2010.01.108
Autor:
Virginia M, Tanis, Genesis M, Bacani, Jonathan M, Blevitt, Christa C, Chrovian, Shelby, Crawford, Aimee, De Leon, Anne M, Fourie, Laurent, Gomez, Cheryl A, Grice, Krystal, Herman, Aaron M, Kearney, Adrienne M, Landry-Bayle, Alice, Lee-Dutra, Jay, Nelson, Jason P, Riley, Alejandro, Santillán, John J M, Wiener, Xiaohua, Xue, Arlene L, Young
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(24)
Previously, benzthiazole containing LTA(4)H inhibitors were discovered that were potent (1-3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering cLogD) a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::acc689db16d005c56ec392d77c4f18cc
https://pubmed.ncbi.nlm.nih.gov/23127888
https://pubmed.ncbi.nlm.nih.gov/23127888
Publikováno v:
Anti-Inflammatory Drug Discovery ISBN: 9781849734134
Leukotriene A4 hydrolase is a zinc-containing cytosolic enzyme with both hydrolase and aminopeptidase activity. LTA4H stereospecifically catalyzes the transformation of the unstable epoxide LTA4 to the potent pro-inflammatory mediator LTB4. Variation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ae1528630f493ad1aab353493deb8cf1
https://doi.org/10.1039/9781849735346-00058
https://doi.org/10.1039/9781849735346-00058
Autor:
Cheryl A. Grice, Todd K. Jones, Scott D. Bembenek, Lars Karlsson, Siquan Sun, James P. Edwards, Danielle K. Wiener, Alice Lee-Dutra, Steven Nguyen, Robin L. Thurmond
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide functional groups were prepared with the goal of improving upon the cellular activity of amidoethylthioethers. This Letter describes altered amide connectivi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14abdf1b459a78cb27bb1342c3aa2d51
https://pubmed.ncbi.nlm.nih.gov/20188543
https://pubmed.ncbi.nlm.nih.gov/20188543
Autor:
John J. M. Wiener, Siquan Sun, Alvah T. Wickboldt, James P. Edwards, Todd K. Jones, Danielle K. Wiener, Lars Karlsson, Alice Lee-Dutra, Steven Nguyen, Cheryl A. Grice
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
A novel class of tetrahydropyrido-pyrazole thioether amines that display potency against human Cathepsin S have been previously reported. Here, further SAR investigations of the P3, P4, and P5 regions are described. In particular, 4-fluoropiperidine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3457f8050d0fb1f0756733636a9f4d1c
https://pubmed.ncbi.nlm.nih.gov/20171097
https://pubmed.ncbi.nlm.nih.gov/20171097
Autor:
Frank U. Axe, Johnathan C. Buma, Lars Karlsson, Raymond Rynberg, Michael D. Hack, J. Guy Breitenbucher, Jonathan M. Blevitt, Alice Lee-Dutra, Danielle K. Neff, Anders Brunmark
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(23)
A series of benzimidazole compounds containing pendant alcohol and amine moieties was found to be active against checkpoint kinase Chk2. These compounds were prepared to examine a potential hydrogen bond interaction with an active site residue and to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f82bee811cb903470d3cc8f3d7cf9271
https://pubmed.ncbi.nlm.nih.gov/17937984
https://pubmed.ncbi.nlm.nih.gov/17937984
Autor:
Haripada Khatuya, Alice Lee-Dutra, Lars Karlsson, J. Guy Breitenbucher, Steven Nguyen, Kristen L. Arienti, Michael D. Hack, Daniel J. Buzard, Robin L. Thurmond, James P. Edwards, Pragnya J. Desai
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(23)
A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure–activity relationships were investigated through library preparation and evaluation as well as traditional medicinal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed016a6695b58c68f62f3fe9a6cc4ac6
https://pubmed.ncbi.nlm.nih.gov/16990005
https://pubmed.ncbi.nlm.nih.gov/16990005