Zobrazeno 1 - 10
of 78
pro vyhledávání: '"Todd K. Jones"'
Autor:
Gary P. O'Neill, Todd K. Jones, Olivia D. Weber, Cheryl A. Grice, Cassandra L. Henry, Justin S. Cisar, Jacqueline L. Blankman, Jessica P. Alexander, R. Alan B. Ezekowitz, Jason R. Clapper, Gabriel M. Simon
Publikováno v:
Journal of medicinal chemistry. 61(20)
The serine hydrolase monoacylglycerol lipase (MGLL) converts the endogenous cannabinoid receptor agonist 2-arachidonoylglycerol (2-AG) and other monoacylglycerols into fatty acids and glycerol. Genetic or pharmacological inactivation of MGLL leads to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe3392790c41c15f6717038b3ed265c3
https://pubmed.ncbi.nlm.nih.gov/30067909
https://pubmed.ncbi.nlm.nih.gov/30067909
Autor:
Gabriel M. Simon, Cheryl A. Grice, Micah J. Niphakis, Olivia D. Weber, R. Alan B. Ezekowitz, Nhi Ngo, Rachel A. Herbst, Jason R. Clapper, Justin S. Cisar, Iain P. Fraser, Jacqueline L. Blankman, Dylan M. Herbst, Mark L. Cunningham, Gary P. O'Neill, Todd K. Jones, Anna M. Knize, Alex Reed, Cassandra L. Henry, Aundrea R. Coppola, Andreu Viader, Jessica P. Alexander
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 367(3)
Monoacylglycerol lipase (MGLL) is the primary degradative enzyme for the endocannabinoid 2-arachidonoylglycerol (2-AG). The first MGLL inhibitors have recently entered clinical development for the treatment of neurologic disorders. To support this cl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef38160293a49bd7fff58ad8eba72dc0
https://pubmed.ncbi.nlm.nih.gov/30305428
https://pubmed.ncbi.nlm.nih.gov/30305428
Autor:
Michael D. Hack, Andrew Skalkin, Peter Ten Holte, Dimitris K. Agrafiotis, Mark Seierstad, Christophe Buyck, Dmitrii N. Rassokhin, Taraneh Mirzadegan, Todd K. Jones
Publikováno v:
Journal of Chemical Information and Modeling. 51:3275-3286
We present a novel approach for enhancing the diversity of a chemical library rooted on the theory of the wisdom of crowds. Our approach was motivated by a desire to tap into the collective experience of our global medicinal chemistry community and i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::579aceb1661c32a26939f2875c9a9be5
https://doi.org/10.1021/ci200446y
https://doi.org/10.1021/ci200446y
Autor:
Christopher M. Mapes, Shirin Shinde, Kelly J. McClure, Laurent Gomez, J. Guy Breitenbucher, Todd K. Jones, Clark A. Sehon, Neelakandha S. Mani, Marna C. W. Pippel, Xiaohu Deng, Chennagiri R. Pandit
Publikováno v:
The Journal of Organic Chemistry. 75:7950-7953
We describe a practical and scalable route to compound (Z)-1, a selective CCK1 receptor antagonist. Notable features of this concise route are (1) a regioselective construction of the pyrazole core through the reaction of an aryl hydrazine and an ela
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13646b1c64bcf2dff772564571602c82
https://doi.org/10.1021/jo1017684
https://doi.org/10.1021/jo1017684
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:
Alejandro Santillan, John J. M. Wiener, Brian J. Morrow, Jiejun Wu, Todd K. Jones, Wolin Ronald L, Pippel Daniel J, Laurent Gomez, Michael D. Hack, Karen Joy Shaw, S. Timothy Motley, Neelakandha S. Mani, Hari Venkatesan, Cheryl A. Grice
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2723-2727
In an attempt to search for a new class of antibacterial agents, we have discovered a series of pyrazole analogs that possess good antibacterial activity for Gram-positive and Gram-negative organisms via inhibition of type II bacterial topoisomerases
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c31291ac440ad7e1597b77822253efc
https://doi.org/10.1016/j.bmcl.2007.03.003
https://doi.org/10.1016/j.bmcl.2007.03.003
Autor:
Alejandro Santillan, Hariharan Venkatesan, Michael D. Hack, Laurent Gomez, Todd K. Jones, Cheryl A. Grice, S. Timothy Motley, John J. M. Wiener, Raul Goldschmidt, Shirin Shinde, Karen Joy Shaw, Brian J. Morrow, Kimberly L. Schwarz, Brett D. Allison, Liu Tang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2718-2722
We have previously reported a novel class of tetrahydroindazoles that display potency against a variety of Gram-positive and Gram-negative bacteria, potentially via interaction with type II bacterial topoisomerases. Herein are reported SAR investigat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::804edff28c9316a2f0d4257caf38a797
https://doi.org/10.1016/j.bmcl.2007.03.004
https://doi.org/10.1016/j.bmcl.2007.03.004
Autor:
Robert I. Higuchi, Todd K. Jones, Arjan van Oeveren, Barbara Pio, Lin Zhi, Min Wu, Andres Negro-Vilar, Christopher M. Tegley, Keith B. Marschke
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1523-1526
A series of alkylamino-2-quinolinone compounds (3) was discovered as androgen receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to androgen receptor and potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0049481585dbb5d66ebe1f96b6191278
https://doi.org/10.1016/j.bmcl.2007.01.007
https://doi.org/10.1016/j.bmcl.2007.01.007
Publikováno v:
The Journal of Organic Chemistry. 71:5039-5042
An efficient method for the stereoselective synthesis of (Z)-α-arylacrylates is described. Treatment of α-hydroxyesters with triflic anhydride and pyridine at 0 °C followed by warming to room temperature afforded the corresponding (Z)-α-aryl-α,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a987f5f8c04c144361926dcf3ea90446
https://doi.org/10.1021/jo060586t
https://doi.org/10.1021/jo060586t
Autor:
William Charles Ripka, Scott W. Nelson, Kevin M. Short, Michael J. Newman, Richard B. Honzatko, Karl Norvell, Frank U. Axe, Kristen L. Arienti, Deborah H. Slee, Tassie L. Collins, Todd K. Jones, Jun-young Choe, Herbert J. Fromm, Rachel Denise Anne Kimmich, Suzanne J. Romano
Publikováno v:
Journal of Biological Chemistry. 278:51176-51183
A highly constrained pseudo-tetrapeptide (OC252-324) further defines a new allosteric binding site located near the center of fructose-1,6-bisphosphatase. In a crystal structure, pairs of inhibitory molecules bind to opposite faces of the enzyme tetr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ea24c33701eda690081ee60805f1970
https://doi.org/10.1074/jbc.m308396200
https://doi.org/10.1074/jbc.m308396200