Allosteric GABAA Receptor Modulators-A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

被引：20

作者：

Alanis, Blanca Angelica Vega ^{[1
]}

Iorio, Maria Teresa ^{[1
]}

Silva, Luca L. ^{[2
]}

Bampali, Konstantina ^{[3
]}

Ernst, Margot ^{[3
]}

Schnuerch, Michael ^{[1
]}

Mihovilovic, Marko D. ^{[1
]}

机构：

[1] TU Wien, Inst Appl Synthet Chem, Getreidemarkt 9-193, A-1060 Vienna, Austria

[2] Charite, Dept Anesthesiol & Intens Care Med, Charitepl 1, D-10117 Berlin, Germany

[3] Med Univ Vienna, Ctr Brain Res, Dept Mol Neurosci, Spitalgasse 4, A-1090 Vienna, Austria

来源：

MOLECULES | 2020年 / 25卷 / 04期

基金：

奥地利科学基金会;

关键词：

GABA(A) modulators; allosteric modulators; heterocyclic modulators; heterocyclic synthesis; nitrogen heterocycles; GAMMA-AMINOBUTYRIC-ACID; HIGH-AFFINITY; IN-VITRO; BENZODIAZEPINE SITE; PHARMACOKINETIC PROPERTIES; ANTICONVULSANT ACTIVITY; INTERNATIONAL UNION; BIOLOGICAL-ACTIVITY; EFFICIENT SYNTHESIS; SELECTIVE LIGANDS;

D O I：

10.3390/molecules25040999

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

GABA(A) receptor modulators are structurally almost as diverse as their target protein. A plethora of heterocyclic scaffolds has been described as modulating this extremely important receptor family. Some made it into clinical trials and, even on the market, some were dismissed. This review focuses on the synthetic accessibility and potential for library synthesis of GABA(A) receptor modulators containing at least one heterocyclic scaffold, which were disclosed within the last 10 years.

引用

页数：47

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