Cerebroprotective Activity of New Derivatives of Pirimidine4 1h  One Pir9 and Pir10 in Irreversible Occlusion of the Common Carotid Artery

Nowadays, the incidence of cerebrovascular disease is steadily increasing. Disorders of cerebral circulation contribute to the increase in the degree of mortality, disability, and incapacitation of the population. An extensive arsenal of drugs with cerebroprotective effects does not satisfy clinical specialists. In this connection, there is an obvious need for new compounds exhibiting cerebroprotropic properties, as well as those able of improving the prognosis of the course of ischemic genesis pathologies.The aimof the article is to study the dose-dependent cerebrotropic effect of a pyrimidine derivative under PIR-9 code against the background of experimental cerebral ischemia in rats.Materials and methods. The experiment was conducted on 140 male Wistar rats (m=170–190 g) divided into 7 equal groups. Pyrimidine derivative PIR – 9 (25, 50 and 100 mg/kg), Vinpocetine (3.2 mg/kg) and Cinnarizine (5.6 mg/kg) suspension of purified water and Tween-80 were used as the studied substances. Experimental cerebral ischemia was reproduced by irreversible occlusion of common carotid arteries (chloral hydrate anesthesia – 350 mg/kg). Experimental substances, reference preparations and purified water were administered prophylactically within 10 days before surgery. One day later the survival, neurological deficiency, behavioral activity, changes in cognitive-mnestic functions, as well as some indicators of brain energy exchange were evaluated.Results.In an experimental study of the cerebrotropic effect of the substance under PIR-9 code (pyrimidine-4-(1H)-one derivative) in various dosages against the background of irreversible occlusion of the common carotid arteries, a decrease in neurological, behavioral, mnestic and cognitive defects has been established. Hereby, the best effect was observed against the background of the administration of the compound PIR-9 at the dose of 50 mg kg. In addition, the prophylactic administration of the test substance PIR-9 (50 mg/kg) has shown the improvement of the energy metabolism in the postischemic period.Conclusion. In the course of the study it was established that the substance under the laboratory code PIR-9 exhibited the most pronounced cerebroprotective effect at the dose of 50 mg/ kg, which was not inferior in its strength to the reference drug Cinnarizine and exceeding Vinpocetine.

show abstract

Study of Cerebrotropic Dose-Dependent Effect of Pyrimidine Derivative Under Pir-9 Code Against the Background of Experimental Cerebral Ischemia in Rats

Voronkov

Шабанова

Воронкова

et al. 2019

Farm. farmakol. (Pâtigorsk)

Self Cite

View full text Add to dashboard Cite

show abstract

Dialkyl Isomers of Benzenesulfonamidphenylpyrimidine-4(1h)-One: Synthesis, Structure and Pharmacological Studies

Anenko,

Kodonidi,

Kirik

et al. 2024

IND. DRU.

View full text Add to dashboard Cite

Interaction of N-acetyl-2-phenylacetamide with sulfanilamide and N-(2-phenylacetyl)propanamide with sulfanilamide led to the preparation of the two isomeric benzenesulfonamidphenylpyrimidin-4(1H)-ones. In positions 2 and 6, the synthesized phenylpyrimidin-4(1H)-ones contained methyl and ethyl as substituents in the first case (IIa), and ethyl and methyl – in the second one (IIb), respectively. The crystal structures of the compounds have been determined by X-ray powder diffraction. It has been established that the positions of substituents significantly affect the conformation of molecules. In molecule IIa, the phenyl ring is rotated to the pyrimidine one by 84°; in IIb, the both rings lie in the same plane. Due to different conformations, the packing of molecules in the crystal lattice changes significantly. Pharmacological properties of isomeric pyrimidinones have been studied in relation to the anti-inflammatory and cerebroprotective activity in chronic traumatic encephalopathy. A comparative analysis of the drug similarity has been carried out. Screening of anti-inflammatory and cerebroprotective activities has shown that compound IIa surpassed its structural isomer in the pharmacological action, which was interpreted as a greater elasticity result of molecule IIa compared to IIb due to the less extended π-system.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Cerebroprotective Activity of New Derivatives of Pirimidine4 1h One Pir9 and Pir10 in Irreversible Occlusion of the Common Carotid Artery

Cited by 2 publications

References 2 publications

Study of Cerebrotropic Dose-Dependent Effect of Pyrimidine Derivative Under Pir-9 Code Against the Background of Experimental Cerebral Ischemia in Rats

Study of Cerebrotropic Dose-Dependent Effect of Pyrimidine Derivative Under Pir-9 Code Against the Background of Experimental Cerebral Ischemia in Rats

Dialkyl Isomers of Benzenesulfonamidphenylpyrimidine-4(1h)-One: Synthesis, Structure and Pharmacological Studies

Contact Info

Product

Resources

About