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变构γ-氨基丁酸受体调节剂——关于最新杂环化学类型及其合成可及性的综述

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

作者信息

Vega Alanis Blanca Angelica, Iorio Maria Teresa, Silva Luca L, Bampali Konstantina, Ernst Margot, Schnürch Michael, Mihovilovic Marko D

机构信息

Institute of Applied Synthetic Chemistry, TU Wien, Getreidemarkt 9/193, 1060 Vienna, Austria.

Department of Anesthesiology and Intensive Care Medicine, Charité-Universitätsmedizin, Charitéplatz 1, 10117 Berlin, Germany.

出版信息

Molecules. 2020 Feb 24;25(4):999. doi: 10.3390/molecules25040999.

DOI:10.3390/molecules25040999
PMID:32102309
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7070463/
Abstract

GABA 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 receptor modulators containing at least one heterocyclic scaffold, which were disclosed within the last 10 years.

摘要

γ-氨基丁酸（GABA）受体调节剂在结构上几乎与它们的靶蛋白一样多样。大量的杂环骨架已被描述为可调节这个极其重要的受体家族。一些进入了临床试验，甚至上市了，但也有一些被淘汰。本综述聚焦于过去10年内公开的、含有至少一个杂环骨架的GABA受体调节剂的合成可及性及文库合成潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/67ef59eb8ef6/molecules-25-00999-sch009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/b4fafc2908d5/molecules-25-00999-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/145c56c046fb/molecules-25-00999-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/a9cb1445bc50/molecules-25-00999-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/84f0f0521d95/molecules-25-00999-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/d6a17298bac2/molecules-25-00999-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/2d899c1355c0/molecules-25-00999-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/fb83a8571f1d/molecules-25-00999-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/e312ea5d310e/molecules-25-00999-sch003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/68ffbae81142/molecules-25-00999-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/9bd6c6e7722c/molecules-25-00999-sch005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/eefc8e6c29d6/molecules-25-00999-sch006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/40089f13358d/molecules-25-00999-sch007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/fe46bdf707cc/molecules-25-00999-sch008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/67ef59eb8ef6/molecules-25-00999-sch009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/b4fafc2908d5/molecules-25-00999-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/145c56c046fb/molecules-25-00999-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/a9cb1445bc50/molecules-25-00999-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/84f0f0521d95/molecules-25-00999-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/d6a17298bac2/molecules-25-00999-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/2d899c1355c0/molecules-25-00999-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/fb83a8571f1d/molecules-25-00999-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/e312ea5d310e/molecules-25-00999-sch003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/68ffbae81142/molecules-25-00999-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/9bd6c6e7722c/molecules-25-00999-sch005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/eefc8e6c29d6/molecules-25-00999-sch006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/40089f13358d/molecules-25-00999-sch007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/fe46bdf707cc/molecules-25-00999-sch008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a86/7070463/67ef59eb8ef6/molecules-25-00999-sch009.jpg

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