التفاصيل البيبلوغرافية
| العنوان: |
Synthesis and Biological Assessment of 4,1-Benzothiazepines with Neuroprotective Activity on the Ca 2+ Overload for the Treatment of Neurodegenerative Diseases and Stroke. |
| المؤلفون: |
Viejo, Lucía, Rubio-Alarcón, Marcos, Arribas, Raquel L., Moreno-Castro, Manuel, Pérez-Marín, Raquel, Braun-Cornejo, María, Estrada-Valencia, Martín, de los Ríos, Cristóbal |
| المصدر: |
Molecules; Aug2021, Vol. 26 Issue 15, p4473-4473, 1p |
| مصطلحات موضوعية: |
BIOSYNTHESIS, NEURODEGENERATION, THERAPEUTICS, NEUROPROTECTIVE agents, CYTOSOL, TRIAZINE derivatives |
| مصطلحات جغرافية: |
PAMPAS (Argentina) |
| مستخلص: |
In excitable cells, mitochondria play a key role in the regulation of the cytosolic Ca2+ levels. A dysregulation of the mitochondrial Ca2+ buffering machinery derives in serious pathologies, where neurodegenerative diseases highlight. Since the mitochondrial Na+/Ca2+ exchanger (NCLX) is the principal efflux pathway of Ca2+ to the cytosol, drugs capable of blocking NCLX have been proposed to act as neuroprotectants in neuronal damage scenarios exacerbated by Ca2+ overload. In our search of optimized NCLX blockers with augmented drug-likeness, we herein describe the synthesis and pharmacological characterization of new benzothiazepines analogues to the first-in-class NCLX blocker CGP37157 and its further derivative ITH12575, synthesized by our research group. As a result, we found two new compounds with an increased neuroprotective activity, neuronal Ca2+ regulatory activity and improved drug-likeness and pharmacokinetic properties, such as clog p or brain permeability, measured by PAMPA experiments. [ABSTRACT FROM AUTHOR] |
|
Copyright of Molecules is the property of MDPI and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) |
| قاعدة البيانات: |
Complementary Index |
Full Text Finder