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

BA Vega Alanis, MT Iorio, LL Silva, K Bampali, M Ernst… - Molecules, 2020 - mdpi.com
BA Vega Alanis, MT Iorio, LL Silva, K Bampali, M Ernst, M Schnürch, MD Mihovilovic
Molecules, 2020mdpi.com
GABAA 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 GABAA receptor modulators containing at least one heterocyclic scaffold, which
were disclosed within the last 10 years.
GABAA 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 GABAA receptor modulators containing at least one heterocyclic scaffold, which were disclosed within the last 10 years.
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