Synthetic Route of C12H8BrN3OOn November 15, 2010 ,《The rational design of a novel potent analogue of the 5′-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Machrouhi, Fouzia; Ouhamou, Nouara; Laderoute, Keith; Calaoagan, Joy; Bukhtiyarova, Marina; Ehrlich, Paula J.; Klon, Anthony E.. The article conveys some information:
We have designed and synthesized analogs of compound C, [4-(2-piperidinyl-1-ylethoxy)phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine, a non-specific inhibitor of 5′-AMP-activated protein kinase (AMPK), using a computational fragment-based drug design (FBDD) approach. Synthesizing only twenty-seven analogs yielded a compound that was equipotent to compound C in the inhibition of the human AMPK (hAMPK) α2 subunit in the heterotrimeric complex in vitro, exhibited significantly improved selectivity against a subset of relevant kinases, and demonstrated enhanced cellular inhibition of AMPK. The experimental process involved the reaction of 4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4Synthetic Route of C12H8BrN3O)
4-(3-Bromopyrazolo[1,5-a]pyrimidin-6-yl)phenol(cas: 945376-95-4) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Synthetic Route of C12H8BrN3O
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics