TY  - JOUR
AU  - Ma, X
AU  - Lubin, H
AU  - Ioja, Enikő
AU  - Kékesi, Orsolya Sára
AU  - Simon, Ágnes
AU  - Apáti, Ágota
AU  - Orbán, Tamás I.
AU  - Héja, László
AU  - Kardos, Julianna
AU  - Marko, IE
TI  - Straightforward and effective synthesis of gamma-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes
JF  - BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
J2  - BIOORG MED CHEM LETT
VL  - 26
PY  - 2016
IS  - 2
SP  - 417
EP  - 423
PG  - 7
SN  - 0960-894X
DO  - 10.1016/j.bmcl.2015.11.100
UR  - https://m2.mtmt.hu/api/publication/2988827
ID  - 2988827
AB  - Supply of major metabolites such as gamma-aminobutyric acid (GABA), beta-alanine and taurine is an essential instrument that shapes signalling, proper cell functioning and survival in the brain and peripheral organs. This background motivates the synthesis of novel classes of compounds regulating their selective transport through various fluid-organ barriers via the low-affinity gamma-aminobutyric acid (GABA) transporter subtype 2 (GAT2). Natural and synthetic spirocyclic compounds or therapeutics with a range of structures and biological activity are increasingly recognised in this regard. Based on pre-validated GABA transport activity, straightforward and efficient synthesis method was developed to provide an azaspiro[4.5]decane scaffold, holding a variety of charge, substituent and 3D constrain of spirocyclic amine. Investigation of the azaspiro[4.5]decane scaffold in cell lines expressing the four GABA transporter subtypes led to the discovery of a subclass of a GAT2-selective compounds with acyl-substituted azaspiro[4.5]decane core.
LA  - English
DB  - MTMT
ER  -