Bioisosteric Analogues of Cinnamic Acid as Effective Neuroprotectors

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M.E. Neganova
V. Semenov
M. Semenova
O.M. Redkozubova
Yu.R. Aleksandrova
E.A. Lysova
S.G. Klochkov
E.F. Shevtsova


Compounds that act on mitochondrial functions are considered as promising drugs for the treatment of neurodegenerative diseases and age-related dementias. As a basis for the creation of such potential drugs, bioisosteric cinnamic acid analogs and polymethoxybenzene derivatives were selected. Derivatives of cinnamic acid have a wide range of biological activities, which can be important for drugs aimed at the treatment of neurodegenerative diseases, in particular Alzheimer′s disease. In this work, the neuroprotective activity of bioisosteric cinnamic acid analogs and polymethoxybenzene derivatives was studied. Among the compounds studied, lead substances 3, 4, and 7 have been identified. These compounds show no intrinsic toxicity and have a neuroprotective effect on the cellular model of neurodegeneration associated with calcium stress. The mechanism of their cytoprotective activity is probably due to the influence on mitochondrial functions, because these compounds effectively suppress the calcium-induced process of mitochondrial permeability jump. In addition, one of the substances investigated (7) has antioxidant properties, showing the ability to inhibit lipid peroxidation (LPO) of rat brain homogenate, which may be an additional mechanism of neuroprotective effect. The data obtained make it possible to recommend the investigated substances as a basis for the creation of effective neuroprotective drugs capable of influencing early stages of the development of neurodegenerative diseases.

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How to Cite
Neganova, M., Semenov, V., Semenova, M., Redkozubova, O., Aleksandrova, Y., Lysova, E., Klochkov, S., & Shevtsova, E. (2018). Bioisosteric Analogues of Cinnamic Acid as Effective Neuroprotectors. Biomedical Chemistry: Research and Methods, 1(3), e00052.


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