Anti-Ischemic Activity of Triamine ALM-802 under Conditions of Endothelial Dysfunction

Барчуков, В. В.; Цорин, И. Б.; Лихошерстов, А. М.; Вититнова, М. Б.; Mokrov, G. V.; Gudasheva, T. A.; Крыжановский, С. А.

doi:10.1007/s10517-019-04549-2

Cited by 7 publications

(2 citation statements)

References 12 publications

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“…showed a pronounced anti-ischemic effect in animals with endothelial dysfunction. [321] The study of the mechanism of ALM-802 cardioprotective action made it possible to confirm the hypothesis of its multitargeting. ALM-802 blocks voltage-dependent Na + -channels (IC 50 = 94 ± 4 µM) and K +channels (IC 50 = 67 ± 3 µM).…”

Section: Lbc Cardioprotectors From Zakusov Institutementioning

confidence: 95%

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Linked biaromatic compounds as cardioprotective agents

Mokrov

2021

Archiv der Pharmazie

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Cardiovascular diseases (CVDs) are widespread in the modern world, and their number is constantly growing. For a long time, CVDs have been the leading cause of morbidity and mortality worldwide. Drugs for the treatment of CVD have been developed almost since the beginning of the 20th century, and a large number of effective cardioprotective agents of various classes have been created. Nevertheless, the need for the design and development of new safe drugs for the treatment of CVD remains. Literature data indicate that a huge number of cardioprotective agents of various generations and mechanisms correspond to a single generalized pharmacophore model containing two aromatic nuclei linked by a linear linker. In this regard, we put forward a concept for the design of a new generation of cardioprotective agents with a multitarget mechanism of action within the indicated pharmacophore model. This review is devoted to a generalization of the currently known compounds with cardioprotective properties and corresponding to the pharmacophore model of biaromatic compounds linked by a linear linker. Particular attention is paid to the history of the creation of these drugs, approaches to their design, and analysis of the structure-action relationship within each class.

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Section: Lbc Cardioprotectors From Zakusov Institutementioning

confidence: 95%

“…In contrast to the reference drugs trimetazidine (30 mg/kg iv) and ranolazine (10 mg/kg iv), which were effective only in intact rats, compound ALM‐802 (2 mg/kg iv) showed a pronounced anti‐ischemic effect in animals with endothelial dysfunction. [ 321 ]…”

Section: Lbc Cardioprotectors From Zakusov Institutementioning

confidence: 99%