- 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
-
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 = 111 nM, EC50 = 1.78 μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
- 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
-
p. 3983 - 3987
(2013/07/27)
-
- Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: Synthesis and biological testing
-
Novel 4-arylpiperazin-1-yl-substituted 2,3-dihydro-1H-1,4- and 1H-1,5-benzodiazepines and their aza-analogues were synthesized as debenzoclozapine derivatives for evaluation as potential D4-ligands. While Ki values of some of the title compounds came within the range of clozapine, they showed an impressively greater selectivity over other dopamine receptor subtypes, especially D2. For the most promising compounds, intrinsic activity and binding properties to serotonin 5-HT1A and 5-HT2 were also determined.
- Hussenether, Thomas,Huebner, Harald,Gmeiner, Peter,Troschuetz, Reinhard
-
p. 2625 - 2637
(2007/10/03)
-
- Process for the preparation of (3-fluoropyridin-2-yloxy)phenoxypropionic acids
-
(3-Fluoropyridin-2-yloxy)phenoxypropionic acids of formula I STR1 wherein X is hydrogen, fluoro, chloro, bromo or trifluoromethyl and Y is hydrogen, sodium or potassium, are prepared by reacting a compound of formula II STR2 wherein X and Y are as defined for formula I, in an anhydrous mixture of hydrogen fluoride, dimethylsulfoxide and a diazotising agent under normal pressure, and converting the diazonium fluoride so produced by thermal decomposition into the (3-fluoropyridin-2-yloxy)phenoxypropionic acid of formula I.
- -
-
-
- Anti-inflammatory oxazole[4,5-b]pyridines
-
The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.
- -
-
-