Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Kaleen Konrad Childers"'
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors
Autor:
Blair T. Lapointe, Jack D. Scott, Xin Cindy Yan, Haiqun Tang, Janice D Woodhouse, Kaleen Konrad Childers, Robert Faltus, Erin F. DiMauro, Solomon Kattar, Charles S. Yeung, Ravi Kurukulasuriya, Vladimir Simov, Hakan Gunaydin, Anmol Gulati, Joey L. Methot, Rachel L. Palte, Ellen C. Minnihan, Greg Morriello, J. Michael Ellis, Harold B. Wood, Santhosh Neelamkavil, Karin M. Otte, Michael J. Ardolino, Barbara Pio, Ping Liu, Laxminarayan G Hegde, Matthew J. Fell, Vanessa L. Rada, Peter Fuller, Paul J Ciaccio
Publikováno v:
RSC Med Chem
The discovery of potent, kinome selective, brain penetrant LRRK2 inhibitors is the focus of extensive research seeking new, disease-modifying treatments for Parkinson's disease (PD). Herein, we describe the discovery and evolution of a picolinamide-d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c8d45ea7dd7adda70471298a4476afa
https://europepmc.org/articles/PMC8292993/
https://europepmc.org/articles/PMC8292993/
Autor:
Matthew G. Stanton, Sanjeev Munshi, Ian W. Davies, Kaleen Konrad Childers, Michael Hutton, Lee Warren, Mansuo Hayashi, Anna A. Zabierek, Alan B. Northrup, Alexander A. Szewczak, Hugh Nuthall, Andrew M. Haidle, Ben Munoz, Dapeng Chen, Hua-Poo Su, Yongquan Hou, Jason D. Katz, Andreas Harsch, Michael D. Altman, James P. Jewell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:114-120
The initial structure activity relationships around an isoindoline uHTS hit will be described. Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. These efforts allowed for
Autor:
Andrew M. Haidle, Alan B. Northrup, Alexander A. Szewczak, Lee Warren, Jason D. Katz, James P. Jewell, Mansuo Hayashi, Hugh Nuthall, Andreas Harsch, Michael D. Altman, Ian W. Davies, Dapeng Chen, Kaleen Konrad Childers, Michael Hutton, Anna A. Zabierek, Matthew G. Stanton, Yongquan Hou, Ben Munoz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:109-113
Attempts to optimize pharmacokinetic properties in a promising series of pyrrolopyrimidinone MARK inhibitors for the treatment of Alzheimer's disease are described. A focus on physical properties and ligand efficiency while prosecuting this series af
Autor:
Kaleen Konrad Childers, J. Patrick Rogers, Eric Romeo, Andrew M. Haidle, Michelle R. Machacek
Publikováno v:
Tetrahedron Letters. 54:2506-2510
A novel multi-component reaction has been developed for the synthesis of fully substituted 5-amino-4-carboxamidthiazoles. Condensation of an aldehyde with commercially available 2-amino-2-cyanoacetamide in the presence of elemental sulfur and base af
Autor:
Thomas S. Rush, Lin Xu, Paul Tempest, Grace Chan, Eric Bachman, Melaney Bouthillette, Craig Rosenstein, Anjili Mathur, Anna A. Zabierek, Andrew M. Haidle, Kaleen Konrad Childers, Jonathan R. Young, Jan-Rung Mo, Michael D. Altman, C. Gary Marshall
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(8)
A series of carboxamide-substituted thiophenes demonstrating inhibition of JAK2 is described. Development of this chemical series began with the bioisosteric replacement of a urea substituent by a pyridyl ring. Issues of chemical and metabolic stabil
Autor:
Michelle R. Machacek, Eric Romeo, Kaleen Konrad Childers, J. Patrick Rogers, Andrew M. Haidle
Publikováno v:
ChemInform. 44
Various target compounds, intermediates in the preparation of pharmacologically active substances, are directly obtained by base-promoted condensation of 2-amido-2-cyanoacetamide (I) with a variety of aldehydes in the presence of elemental sulfur.