Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors
2013
Chun, Kwangwoo | Park, Ji Seon | Lee, Han-Chang | Kim, Young-Ha | Ye, In-Hea | Kim, Kang-Jeon | Ku, Il-Whea | Noh, Min-Young | Cho, Goang-Won | Kim, Heejaung | Kim, Seung-Hyun | Kim, Jeongmin
New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC₅₀=111nM, EC₅₀=1.78μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
Show more [+] Less [-]AGROVOC Keywords
Bibliographic information
This bibliographic record has been provided by National Agricultural Library