4353-52-0Relevant academic research and scientific papers
In Vitro and in Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas
Ottavi, Samantha,Scarry, Sarah M.,Mosior, John,Ling, Yan,Roberts, Julia,Singh, Amrita,Zhang, David,Goullieux, Laurent,Roubert, Christine,Bacqué, Eric,Lagiakos, H. Rachel,Vendome, Jeremie,Moraca, Francesca,Li, Kelin,Perkowski, Andrew J.,Ramesh, Remya,Bowler, Matthew M.,Tracy, William,Feher, Victoria A.,Sacchettini, James C.,Gold, Ben S.,Nathan, Carl F.,Aubé, Jeffrey
supporting information, p. 1996 - 2022 (2022/01/31)
A newly validated target for tuberculosis treatment is phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. The structure-activity relat
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
Blake, James F.,Gaudino, John J.,De Meese, Jason,Mohr, Peter,Chicarelli, Mark,Tian, Hongqi,Garrey, Rustam,Thomas, Allen,Siedem, Christopher S.,Welch, Michael B.,Kolakowski, Gabrielle,Kaus, Robert,Burkard, Michael,Martinson, Matthew,Chen, Huifen,Dean, Brian,Dudley, Danette A.,Gould, Stephen E.,Pacheco, Patricia,Shahidi-Latham, Sheerin,Wang, Weiru,West, Kristina,Yin, Jianping,Moffat, John,Schwarz, Jacob B.
, p. 2635 - 2639 (2014/06/09)
The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
Blake, James F.,Gaudino, John J.,De Meese, Jason,Mohr, Peter,Chicarelli, Mark,Tian, Hongqi,Garrey, Rustam,Thomas, Allen,Siedem, Christopher S.,Welch, Michael B.,Kolakowski, Gabrielle,Kaus, Robert,Burkard, Michael,Martinson, Matthew,Chen, Huifen,Dean, Brian,Dudley, Danette A.,Gould, Stephen E.,Pacheco, Patricia,Shahidi-Latham, Sheerin,Wang, Weiru,West, Kristina,Yin, Jianping,Moffat, John,Schwarz, Jacob B.
, p. 2635 - 2639 (2015/02/19)
The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.
PROCESS FOR STRAIGHTENING KERATIN FIBRES WITH A HEATING MEANS AND DENATURING AGENTS
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, (2010/03/02)
The invention relates to a process for straightening keratin fibres, comprising: (i) a step in which a straightening composition containing at least two denaturing agents is applied to the keratin fibres, (ii) a step in which the temperature of the keratin fibres is raised, using a heating means, to a temperature of between 110 and 250° C.
Amidination of amines under microwave conditions using recyclable polymer-bound 1H-pyrazole-1-carboxamidine
Solodenko, Wladimir,Broeker, Patrick,Messinger, Josef,Schoen, Uwe,Kirschning, Andreas
, p. 461 - 466 (2007/10/03)
A convenient one-step transformation of primary and secondary amines into the corresponding unprotected guanidines using 4-benzyl-3,5-dimethyl-1H- pyrazole-1-carboxamidine and its polymer-bound variant is described. The scopes and limitations of the method, the microwave-assistance of amidination as well as a recycling protocol are examined. Georg Thieme Verlag Stuttgart.
A new reagent and its polymer-supported variant for the amidination of amines
Dr?ger, Gerald,Solodenko, Wladimir,Messinger, Josef,Sch?n, Uwe,Kirschning, Andreas
, p. 1401 - 1403 (2007/10/03)
New reagents for the high yielding amidination of primary and secondary amines are described. By attaching a benzyl substituent to the 3,5-dimethyl-1H-pyrazole-1-carboxamidine ring, a reagent 1 is obtained which allows easy work-up after amidination because of solubility of byproducts in organic solvents. In addition, the polystyrene-bound analogue 2 was prepared which allows amidination of various amines with high purity.
