Hansen, Stinne W. published the artcileIdentification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study, Application of Methyl 2-(3-formyl-4-hydroxyphenyl)acetate, the publication is Journal of Medicinal Chemistry (2016), 59(19), 8757-8770, database is CAplus and MEDLINE.
Screening of a small compound library at three excitatory amino acid transporter subtypes 1-3 (EAAT1-3) subtypes resulted in the identification of compound (I) that exhibited a distinct preference as an inhibitor at EAAT1 (IC50 20 μM) compared to EAAT2 and EAAT3 (IC50 > 300 μM). This prompted us to subject I to an elaborate structure-activity-relationship study through the purchase and synthesis and subsequent pharmacol. characterization of a total of 36 analogs. Although this effort did not result in analogs with substantially improved inhibitory potencies at EAAT1 compared to that displayed by the hit, it provided a detailed insight into structural requirements for EAAT1 activity of this scaffold. The discovery of this new class of EAAT1-selective inhibitors not only supplements the currently available pharmacol. tools in the EAAT field, but also substantiates the notion that EAAT ligands not derived from α-amino acids hold considerable potential in terms of subtype-selective modulation.
Journal of Medicinal Chemistry published new progress about 61874-04-2. 61874-04-2 belongs to esters-buliding-blocks, auxiliary class Benzene,Phenol,Ester,Aldehyde, name is Methyl 2-(3-formyl-4-hydroxyphenyl)acetate, and the molecular formula is C10H10O4, Application of Methyl 2-(3-formyl-4-hydroxyphenyl)acetate.
Referemce:
https://en.wikipedia.org/wiki/Ester,
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