7364-27-4Relevant articles and documents
Discovery of isatin and 1H-indazol-3-ol derivatives as D-amino acid oxidase (DAAO) inhibitors
Szilágyi, Bence,Kovács, Péter,Ferenczy, Gy?rgy G.,Rácz, Anita,Németh, Krisztina,Visy, Júlia,Szabó, Pál,Ilas, Janez,Balogh, Gy?rgy T.,Monostory, Katalin,Vincze, István,Tábi, Tamás,Sz?k?, éva,Keser?, Gy?rgy M.
, p. 1579 - 1587 (2018/02/23)
D-Amino acid oxidase (DAAO) is a potential target in the treatment of schizophrenia as its inhibition increases brain D-serine level and thus contributes to NMDA receptor activation. Inhibitors of DAAO were sought testing [6+5] type heterocycles and identified isatin derivatives as micromolar DAAO inhibitors. A pharmacophore and structure-activity relationship analysis of isatins and reported DAAO inhibitors led us to investigate 1H-indazol-3-ol derivatives and nanomolar inhibitors were identified. The series was further characterized by pKa and isothermal titration calorimetry measurements. Representative compounds exhibited beneficial properties in in vitro metabolic stability and PAMPA assays. 6-fluoro-1H-indazol-3-ol (37) significantly increased plasma D-serine level in an in vivo study on mice. These results show that the 1H-indazol-3-ol series represents a novel class of DAAO inhibitors with the potential to develop drug candidates.
PHARMACEUTICALS CONTAINING NOVEL 1-POSITION SUBSTITUTED INDAZOLE DERIVATIVE
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Paragraph 0121, (2016/10/09)
PROBLEM TO BE SOLVED: To provide pharmaceuticals containing a compound having strong effect of modulating α7 nicotinic acetylcholine receptor (α7nAChR) and useful as treatment agent for diseases related to cholinergic in central nervous system (CNS) and/o
NOVEL 1-SUBSTITUTED INDAZOLE DERIVATIVE
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Paragraph 0228-0230, (2014/05/08)
A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and