Acetoxybenzoylglycylglycines as Potential Cerebroprotective Compounds

Brel, A. K.; Tyurenkov, I. N.; Lisina, S. V.; Попов, С. С.; Verkholyak, D. V.; Budaeva, Yu. N.; Волотова, Е. В.; Atapina, N. V.; Куркин, Д. В.

doi:10.1007/s11094-018-1762-0

Cited by 4 publications

(3 citation statements)

References 1 publication

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“…представляют интерес в качестве потенциальных хемотипов для разработки на их основе церебропротекторных средств, поскольку для некоторых отмечено наличие ноотропной, противогипоксической, эндотелио-и стресспротекторной активности [6,7]. Гидроксибензойные кислоты также привлекают внимание вследствие наличия у них противовоспалительного, антиагрегантного и антиоксидантного действия [8]. В данной работе изложены результаты исследования церебропротекторного действия соединения С40 (коньюгата производного гидроксибензойной кислоты с глицином) (рис.…”

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Neuroprotective action of hydroxybenzoic acid derivative with glycine (C40) in the middle cerebral artery occlusion in rats with chronic cerebral circulation insufficiency

Verkholyak,

Bakulin,

Brel

et al. 2024

Journal of Volgograd State Medical University

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The neuroprotective effect of a novel conjugate of hydroxybenzoic acid with glycine (C40) was investigated in a model of ischemic stroke in rats with chronic cerebral circulation insufficiency (CCCI). The study was conducted in two stages: first, CCCI was modeled by stenosing the common carotid arteries by 50 %, followed by a 60-minute middle cerebral artery occlusion (stroke) after 40 days. Compound C40 and the reference drug citicoline were administered for 10 days before stroke and for 3 days after. Further, neurological deficit (the Garcia and Combs D’Alecy scales), sensorimotor functions (Open Field test, Adhesive Removal test, and Rotarod test), cognitive impairments (Novel Object Recognition and Morris Water Maze tests), cerebral blood flow level, and endothelial function were evaluated. Animals receiving the test substances demonstrated a statistically significant reduction in neurological deficit, less pronounced motor coordination and sensorimotor function impairments, as well as fewer short-term and long-term memory deficits compared to the negative control group. The observed decrease in neurological deficit in the experimental groups was accompanied by improved endothelial function and increased cerebral blood flow. The neuroprotective effect of the novel hydroxybenzoic acid derivative with glycine (C40) was comparable to that of reference drug citicoline.

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Neuroprotective action of hydroxybenzoic acid derivative with glycine (C40) in the middle cerebral artery occlusion in rats with chronic cerebral circulation insufficiency

Verkholyak,

Bakulin,

Brel

et al. 2024

Journal of Volgograd State Medical University

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“…привлекают внимание в качестве потенциальных церебропротекторных средств, поскольку для некоторых отмечено наличие ноотропной, противогипоксической, эндотелио-и стресспротекторной активности [4]. Производные гидроксибензойных кислот также представляют интерес для поиска новых церебропротективных препаратов вследствие наличия у них противовоспалительного, антиагрегантного и антиоксидантного действия [5]. Последние 15 лет волгоградские фармакологи совместно с химиками синтетиками Волгоградского государственного медицинского университета ведут поиск веществ с нейропротективной активностью при цереброваскулярных патологиях среди различных производных нейроактивных аминокислот [5,6].…”

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Influence of N-(4-Acetoxybenzoyl)potassium Glycinate on Sensor-Motor and Cognitive Disordersin Rats With Chroniccerebrovascular Insufficiency

2022

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The effect of a new conjugate of hydroxybenzoic acid with glycine on sensory-motor and cognitive impairments in experimental animals with chronic cerebrovascular insufficiency (CCI) was studied. CCI was modeled in rats by stenosis of the lumen of the carotid arteries in 60 %. 40 days after the operation, experimental groups were formed and the test compound was administered for 14 days. Citicoline was used as a reference drug, and saline was administered as placebo. After treatment with the Rotarod, Adhesion Test, Novel Object Recognition (NOR), and Morris Water Maze tests, the severity of sensory-motor and cognitive impairments was assessed. It was noted that in animals with CCI with placebo treatment, the pathology was accompanied by a pronounced impairment of coordination and sensory-motor function of the forelimbs, as well as cognitive impairments (impaired short-term and long-term memory in the NOR and the Morris maze tests). The course introduction of a new conjugate of hydroxybenzoic acid with glycine contributed to a significant improvement in sensory-motor and cognitive functions in animals with CCI. The noted neuroprotective effect was comparable to that of the reference drug citicoline.

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“…Исследования показали, что новые N-гидроксибензоилацилированные аминокислоты, пептиды и гетероциклические основания, полученные на основе гидроксибензоил хлоридов, являются перспективным лекарственными препаратами для лечения нарушений мозгового кровообращения ишемического генеза, а также в качестве основы для создания средств, подавляющих развитие отсроченных осложнений диабета [2,3], прошедших государственную регистрацию.…”

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Ацилхлориды Гидроксибензойных Кислот И Их Производных Как Полупродукты В Синтезе N-Ацилированных Биологически Активных Соединений

Брель¹,

Лисина²,

Будаева³

et al. 2021

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Acetoxybenzoylglycylglycines as Potential Cerebroprotective Compounds

Cited by 4 publications

References 1 publication

Neuroprotective action of hydroxybenzoic acid derivative with glycine (C40) in the middle cerebral artery occlusion in rats with chronic cerebral circulation insufficiency

Neuroprotective action of hydroxybenzoic acid derivative with glycine (C40) in the middle cerebral artery occlusion in rats with chronic cerebral circulation insufficiency

Influence of N-(4-Acetoxybenzoyl)potassium Glycinate on Sensor-Motor and Cognitive Disordersin Rats With Chroniccerebrovascular Insufficiency

Ацилхлориды Гидроксибензойных Кислот И Их Производных Как Полупродукты В Синтезе N-Ацилированных Биологически Активных Соединений

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