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Vorträge und Posterpräsentationen (ohne Tagungsband-Eintrag):

B. Vega Alanis, L. Wimmer, M. Ernst, M.D. Mihovilovic:
"Synthesis of novel scaffolds as selective ligands for the alpha+/beta- interface of the GABAA receptor";
Poster: 7th Paul Ehrlich MedChem EuroPhD Network Symposium, Vienna; 25.08.2017 - 27.08.2017.



Kurzfassung englisch:
GABAA receptors are the major inhibitory neurotransmitter receptors in the central nervous system. These GABA-gated chloride channels are composed of five subunits that can belong to different subunit classes. Several pyrazoloquinolinone ligands have already been described as high affinity ligands of the
benzodiazepine (Bz) binding site.1,2 In this regard, compound LAU 177 (4-(8-methoxy-3-oxo-3,5-dihydro-2H-pyrazolo[4,3-c]quinolin-2-yl) benzonitrile was evaluated at several ab, abg and abd receptor subtypes. The evidence of this study indicated that LAU 177 exerts its modulatory effect in a1b3, a1b3g2 and a1b3d receptors by binding to the extracellular pocket at the a1+b3- interface.2 In order to obtain further compounds with a higher selectivity towards the a+b- interface, several isosteric replacements were performed, leading to a novel scaffolds. The derivatives of this new scaffold might maintain the same binding mode at the desired interface due to the analogy with the closed structure. The results of this work are here presented and the properties of these compounds will be further investigated.

Erstellt aus der Publikationsdatenbank der Technischen Universität Wien.