Synthesis of New 1,3,4-Thiadiazines Capable of Inhibiting Nonenzymatic Glycosylation of Proteins

Sidorova, L. P.; Цейтлер, Т. А.; Perova, N. M.; Emelyanov, V. V.; Savateeva, E. A.; Maksimova, N. E.; Mochul’skaya, N. N.; Chereshnev, V. А.; Чупахин, О. Н.

doi:10.1007/s11094-015-1314-9

Cited by 9 publications

(5 citation statements)

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“…Thus, it was found that several chemical compounds of the group of substituted thiadiazines possessed the attributes of atypical antipsychotics, having a significant effect on the behavior of animals and the course of the stress reaction [ 54 , 88 ]. Concurrently, this class of compounds had an exceptional breadth on the biological activity spectrum [ 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 ]. Such pleiotropic actions served as the basis for the search for a single mechanism capable of influencing both the course of the inflammatory process and the stress reaction.…”

Section: Discussionmentioning

confidence: 99%

“…Some of the compounds are able to inhibit the non-enzymatic glycosylation of proteins in experiments in vitro [ 51 ] and to cause hypothermia in experiments in vivo [ 52 ]. Several substituted 1,3,4-thiadiazines were provided as anaesthetic, cardiovascular and hypometabolic agents [ 53 ].…”

Section: Methodsmentioning

confidence: 99%

“…In the PubMed and ScienceDirect search engines, no publications were published on the activity of 1,3,4-thiadiazines in myocardial infarction, other than those referenced in this review [ 48 , 49 , 50 , 51 , 52 , 53 , 54 ] (search query “thiadiazine myocardial infarction”).…”

Section: Methodsmentioning

confidence: 99%

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Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

et al. 2018

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This review focuses on the biological action of the compounds from the group of substituted 1,3,4-thiadiazines on stress response and myocardial infarction. The aim of this review is to propose the possible mechanisms of action of 1,3,4-thiadiazines and offer prospectives in the development of new derivatives as therapeutic agents. It is known, that compounds that have biological effects similar to those used as antidepressants can down-regulate the secretion of proinflammatory cytokines, up-regulate the release of anti-inflammatory ones and affect cell recruitment, which allows them to be considered immunomodulators as well. The results of pharmacological evaluation, in silico studies, and in vivo experiments of several compounds from the group of substituted 1,3,4-thiadiazines with antidepressant properties are presented. It is proposed that the cardioprotective effects of substituted 1,3,4-thiadiazines might be explained by the peculiarities of their multi-target action: the ability of the compounds to interact with various types of receptors and transporters of dopaminergic, serotonergic and acetylcholinergic systems and to block the kinase signal pathway PI3K-AKT. The described effects of substituted 1,3,4-thiadiazines suggest that it is necessary to search for a new agents for limiting the peripheral inflammatory/ischemic damage through the entral mechanisms of stress reaction and modifying pro-inflammatory cytokine signaling pathways in the brain.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

et al. 2018

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“…Work on the synthesis of 1,3,4-thiadiazine derivatives has been ongoing for several decades at Ural Federal State University in Russia ( Figure 2 ) [ 26 , 27 , 28 , 29 ].…”

Section: Methodsmentioning

confidence: 99%

Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide

et al. 2016

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Substituted thiadiazines exert a reliable therapeutic effect in treating stress, and a schematic description of their ability to influence all aspects of a stress response has been depicted. This study was conducted to pharmacologically evaluate compound L-17, a substituted thiadiazine, (2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide) for possible anti-psychotic/antidepressant activity. Compound L-17 was synthesized by cyclocondensation of α-bromoacetophenone with the original morpholine-4-carbothionic acid hydrazide. Pharmacologic evaluations were conducted using methods described by E.F. Lavretskaya (1985), and in accordance with published guidelines for studying drugs for neuroleptic activity. Compound L-17 was evaluated for various possible mechanisms of action, including its effects on cholinergic system agonists/antagonists, dopaminergic neurotransmission, the adrenergic system, and 5-HT3 serotonin receptors. One or more of these mechanisms may be responsible for the beneficial effects shown by thiadiazine compounds in experiments conducted to evaluate their activity in models of acute stress and acute myocardial infarction.

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“…Чу-пахина. Как установлено нашими предыдущими исследованиями, эти вещества обладают способ- [15,37]. Нами также была впервые обнаружена способ-ность соединений ряда 1,3,4-тиадиазина корри-гировать течение аллоксанового СД у крыс, что выражалось в снижении гипергликемии, окси-дативного стресса и накопления гликированных белков в крови и органах животных [9,10,12], и установлена минимально необходимая продол-жительность введения соединения ряда 1,3,4-ти-адиазина [11].…”

Section: Introductionunclassified

Cytokine Regulation of Regenerative Processes in Pancreatic Gland in Alloxan-Induced Diabetic Rats, and It Correction by 1,3,4-Thiadiazine Composition and Lipoic Acid

Данилова¹,

Емельянов²,

Гетте³

et al. 2018

Med. immunol.

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Synthesis of New 1,3,4-Thiadiazines Capable of Inhibiting Nonenzymatic Glycosylation of Proteins

Cited by 9 publications

References 5 publications

Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide

Cytokine Regulation of Regenerative Processes in Pancreatic Gland in Alloxan-Induced Diabetic Rats, and It Correction by 1,3,4-Thiadiazine Composition and Lipoic Acid

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