45715-47-7Relevant academic research and scientific papers
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.
Optimisation of the synthesis of guanidines from amines via nitroguanidines using 3,5-dimethyl-N-nitro-1H-pyrazole-1-carboxamidine
Castillo-Melendez, Joel A.,Golding, Bernard T.
, p. 1655 - 1663 (2007/10/03)
The synthesis of the useful reagent for the preparation of guanidines, 3,5-dimethyl-N-nitro-1-pyrazole-1-carboxamidine (DMNPC), has been optimised. A detailed protocol for using this reagent for the preparation in pure form of a range of guanidines via nitroguanidines is described. A comparison has been made regarding efficiency between DMNPC and the guanidinylating reagents N,N′-bis-Boc-1-pyrazole-1-carboxamidine (2) and N,N′-bis-Boc- N′-triflylguanidine (3).
Preparation and diuretic properties of novel amiloride analogues
Russ,Ried,Ullrich,Mutschler
, p. 761 - 767 (2007/10/02)
Fifteen novel amiloride analogues were synthesized and their diuretic properties compared to amiloride and triamterene in white wistar rats. Whereas none of the 6-substituted derivatives exhibited significant natriuretic and antikaliuretic effects, five of the compounds modified in the 2-position were found equal or better than standards. The results are discussed with respect to chemical structure and physicochemical properties.
