Chowdhury, Sarwat; Chen, Yen Ting; Fang, Xingang; Grant, Wayne; Pocas, Jennifer; Cameron, Michael D.; Ruiz, Claudia; Lin, Li; Park, HaJeung; Schroter, Thomas; Bannister, Thomas D.; LoGrasso, Philip V.; Feng, Yangbo published the artcile< Amino acid derived quinazolines as Rock/PKA inhibitors>, Name: 3-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, the main research area is amino acid derived quinazolinone Rock PKA inhibitor.
SAR and lead optimization studies for Rock inhibitors based on amino acid-derived quinazolines are described. Studies demonstrated that these amino acid derived quinazolinones were mainly puromycin aminonucleoside (PAN)-Rho-associated protein kinase (Rock) (I & II) inhibitors. While selectivity against other kinases could be achieved, selectivity for most of these compounds against PKA was not achieved. This is distinct from Rock inhibitors based on non-amino acid derived quinazolinones, where high selectivity against PKA could be obtained.22 The inhibitors presented here in some cases possessed sub-nanomolar inhibition of Rock, nanomolar potency in ppMLC cell based assays, low to fair cytochrome P 450 inhibition, and good human microsomal stability.
Bioorganic & Medicinal Chemistry Letters published new progress about Heteroarylation (Suzuki). 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Name: 3-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics