1.
Chembiochem
; 19(6): 613-621, 2018 03 16.
Artigo
em Inglês
| MEDLINE
| ID: mdl-29314498
RESUMO
We describe the design, synthesis, and structure-activity relationships (SARs) of a series of 2-aminobenzothiazole inhibitors of Rho kinases (ROCKs) 1 and 2, which were optimized to low nanomolar potencies by use of protein kinaseâ A (PKA) as a structure surrogate to guide compound design. A subset of these molecules also showed robust activity in a cell-based myosin phosphatase assay and in a mechanical hyperalgesia in vivo pain model.