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作用于中枢神经系统(CNS)靶点的药物作为非中枢神经系统靶点的先导药物。

Drugs acting on central nervous system (CNS) targets as leads for non-CNS targets.

作者信息

Kharkar Prashant S

机构信息

Department of Pharmaceutical Chemistry, SPP School of Pharmacy and Technology Management, SVKM's NMIMS, Mumbai, 400056, India.

出版信息

F1000Res. 2014 Feb 6;3:40. doi: 10.12688/f1000research.3-40.v2. eCollection 2014.

DOI:10.12688/f1000research.3-40.v2
PMID:24715979
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3961999/
Abstract

Innovative drug discovery approaches are currently needed to rejuvenate the shrinking product pipelines of the pharmaceutical companies across the globe. Here a theme is presented - the use of central nervous system (CNS) drugs as leads for non-CNS targets. The approach is related to the use of existing drugs for new indications. Suitable chemical modifications of the CNS drugs abolish their CNS penetration. These novel analogs may then be screened for activity against non-CNS targets. Careful selection of the appropriate structural modifications remains the key to success.

摘要

目前需要创新的药物发现方法来振兴全球制药公司日益缩减的产品线。本文提出了一个主题——利用中枢神经系统(CNS)药物作为非中枢神经系统靶点的先导物。该方法与将现有药物用于新适应症有关。对中枢神经系统药物进行适当的化学修饰可消除其对中枢神经系统的渗透。然后可以筛选这些新型类似物针对非中枢神经系统靶点的活性。谨慎选择合适的结构修饰仍然是成功的关键。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e27/3968893/aa7af81766d3/f1000research-3-4081-g0000.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e27/3968893/aa7af81766d3/f1000research-3-4081-g0000.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e27/3968893/aa7af81766d3/f1000research-3-4081-g0000.jpg

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