Synthesis and Study of Psychotropic Activity of 1-Substituted 4-Amino-5-oxoprolines

Vigorov, A. Yu.; Краснов, В. П.; Низова, И. А.; Садретдинова, Л. Ш.; Левит, Г. Л.; Матвеева, Т. В.; Слепухин, П. А.; Бакулин, Д. А.; Kovalyov, N. S.; Tyurenkov, I. N.; Charushin, Valery N.

doi:10.1134/s0012500820090049

Cited by 4 publications

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“…We have previously shown that 4-amino-1-aryl-5-oxoprolines and 4-(arylamino)-5oxoprolines exhibit antiplatelet and antithrombotic activity in vitro and in vivo (Figure 2); the best results in this type of activity were shown by (2S,4S)-4-amino-1-(4-fluorophenyl)-5-oxoproline [15,16]. Some derivatives of this series also demonstrated cerebroprotective and psychotropic activity in experiments in vivo [16,17].…”

Section: Chemistrymentioning

confidence: 99%

“…We have previously shown that 4-amino-1-aryl-5-oxoprolines and 4-(arylamino oxoprolines exhibit antiplatelet and antithrombotic activity in vitro and in vivo (Figur the best results in this type of activity were shown by (2S,4S)-4-amino-1-(4-fluorophen 5-oxoproline [15,16]. Some derivatives of this series also demonstrated cerebroprotec and psychotropic activity in experiments in vivo [16,17]. In this work, we synthesized a number of new amides and peptides of 4-aminostituted 5-oxoprolines and tested their antiplatelet and antithrombotic activity in bot vitro and in vivo experiments.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Assessment of Antiplatelet and Antithrombotic Activity of 4-Amino-Substituted 5-Oxoproline Amides and Peptides

Krasnov,

Nizova,

Vigorov

et al. 2023

Molecules

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Venous thromboembolism is a serious problem because it significantly increases the risk of developing vascular complications in elderly patients with obesity or immobilization, cancer, and many other diseases. Thus, there is a need to study new therapeutic strategies, including new medicinal agents for the efficient and safe correction of thrombus disorders. In this work, we have synthesized a number of new amides and peptides of 4-amino-5-oxoprolines and studied their antiplatelet and antithrombotic activity in experiments in vitro and in vivo. It has been found that the newly obtained compounds slow down the process of thrombus formation in a model of arterial and venous thrombosis, without affecting plasma hemostasis parameters. (2S,4S)-4-Amino-1-(4-fluorophenyl)-5-oxoprolyl-(S)-phenylalanine proved to be the most efficient among the studied derivatives. The results obtained indicate the advisability of further studies on 5-oxoproline derivatives in order to design pharmaceutical agents for the prevention and treatment of the consequences of thrombosis.

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Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%