Chowdhury, Sarwat; Sessions, E. Hampton; Pocas, Jennifer R.; Grant, Wayne; Schroeter, Thomas; Lin, Li; Ruiz, Claudia; Cameron, Michael D.; Schuerer, Stephan; LoGrasso, Philip; Bannister, Thomas D.; Feng, Yangbo published the artcile< Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I)>, Formula: C10H17BN2O2, the main research area is azaindolecarboxamide aralkyl preparation Rho kinase inhibitor.
Rho kinase (ROCK) inhibitors are potential therapeutic agents to treat disorders such as hypertension, multiple sclerosis, cancers, and glaucoma. The synthesis, optimization, biol. evaluation of potent indole and 7-azaindole based ROCK inhibitors that have high potency on ROCK (IC50 = 1 nM) with 740-fold selectivity over PKA, such as I. Moreover, I showed very good DMPK properties making it a good candidate for further development. Finally, docking studies with a homol. model of ROCK-II were performed to rationalize the binding mode of these compounds and showed the compounds bound in both orientations to take advantage to H-bonds with Lys-121 of ROCK-II.
Bioorganic & Medicinal Chemistry Letters published new progress about 936250-20-3. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Formula: C10H17BN2O2.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics