Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Michael D. Spengler"'
Autor:
Michael D. Spengler, Ramona Plant, Kaushik Raha, Hong Lin, Hongyi Yu, Cynthia M. Rominger, Ralph A. Rivero, Michael L. Moore, Mary Ann Hardwicke, Michael D. Schaber, Jeanelle McSurdy-Freed, Karl F. Erhard, Juan I. Luengo, Junya Qu
Publikováno v:
ACS Medicinal Chemistry Letters. 4:230-234
A series of novel [3a,4]dihydropyrazolo[1,5a]pyrimidines were identified, which were highly potent and selective inhibitors of PI3Kβ. The template afforded the opportunity to develop novel SAR for both the hinge-binding (R3) and back-pocket (R4) sub
Autor:
Samm T. Portelli, David Lundberg, Emile P. Chen, Mark A. Levy, Michael M. Ben, Keith W. Ward, Michael D. Spengler, Sarah J. Medina, Kelly M. Mahar Doan
Publikováno v:
Biopharmaceutics & Drug Disposition. 24:17-25
This study was conducted to compare the ability of two potential microdialysis perfusates to enhance the recovery of SB-265123, a lipophilic, highly protein-bound compound, both in vitro and in vivo. Initial in vitro experiments established that the
Publikováno v:
International Journal of Antimicrobial Agents. 7:15-21
The in vitro activity of piperacillin alone or titrated with a constant concentration of 4 μg/ml tazobactam was evaluated against 3962 baseline pathogens isolated from 1899 patients enrolled in 9 clinical trial studies in North America. Tazobactam i
Autor:
Hong Lin, Charles B. Davis, Kaushik Raha, Ralph A. Rivero, Michael D. Schaber, Jeanelle McSurdy-Freed, Mary Ann Hardwicke, Karl F. Erhard, James F. Mack, Ren Xie, Michael D. Spengler, Ramona Plant, Cynthia M. Rominger, Junya Qu, Rosanna Tedesco, Jennifer L. Ariazi, Juan I. Luengo, Mark J. Schulz, Michael D. Squire, Christian S. Sherk, Jin Zeng
A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ace88350b0677b6d5e549d1aab456577
https://europepmc.org/articles/PMC4025772/
https://europepmc.org/articles/PMC4025772/
Autor:
Sanchez Robert, Jeanelle McSurdy-Freed, Hongyi Yu, Michael L. Moore, Rosanna Tedesco, Mary Ann Hardwicke, Karl F. Erhard, Ralph A. Rivero, Kaushik Raha, Michael D. Spengler, Juan I. Luengo, Ramona Plant, Hong Lin, Michael D. Schaber, Cynthia M. Rominger
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(9)
A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated pote
Autor:
Michael D. Spengler, Rosanna Tedesco, Sanchez Robert, Michael D. Schaber, Ramona Plant, Hong Lin, Mary Ann Hardwicke, Karl F. Erhard, James F. Mack, Kaushik Raha, Ralph A. Rivero, Cynthia M. Rominger, Juan I. Luengo, Mark J. Schulz, Jeanelle McSurdy-Freed, Ren Xie, Jin J. Zeng
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(6)
A series of PI3K-beta selective inhibitors, imidazo[1,2-a]-pyrimidin-5(1H)-ones, has been rationally designed based on the docking model of the more potent R enantiomer of TGX-221, identified by a chiral separation, in a PI3K-beta homology model. Syn
Publikováno v:
Scopus-Elsevier
Type 1 fimbriae promote enterobacterial adherence to a variety of mammalian cells and are thought to play an important role in the establishment of various extraintestinal infections. Whether or not this adhesin has a role in the pathogenesis of peri
Publikováno v:
Annals of Surgery. 213:253-260
Intraperitoneal (IP) abscesses frequently are composed of aerobes and anaerobes, and, in experimental models, a particulate adjuvant. The environmental changes effected by these components, either singularly or in combination, have not been well defi
Publikováno v:
Journal of Infectious Diseases. 163:644-667
Intraabdominal infections are a major source of morbidity and mortality for the trauma and postoperative patient. Transient peritoneal contamination with bacteria after either intentional or unintentional violation of the gut are common. The effect o
Autor:
Keith W, Ward, Sarah J, Medina, Samm T, Portelli, Kelly M, Mahar Doan, Michael D, Spengler, Michael M, Ben, David, Lundberg, Mark A, Levy, Emile P, Chen
Publikováno v:
Biopharmaceuticsdrug disposition. 24(1)
This study was conducted to compare the ability of two potential microdialysis perfusates to enhance the recovery of SB-265123, a lipophilic, highly protein-bound compound, both in vitro and in vivo. Initial in vitro experiments established that the