Search for Anti-Inflammatory Agents in the Tetrahydropyrido[2,1-B ][1,3,5]-Thiadiazine Series

Bibik, E. Yu.; Yaroshevskaya, Oksana; Девдера, Анна Вадимовна; Деменко, А. В.; Zakharov, V. V.; Фролов, К. А.; Dotsenko, V. V.; Кривоколыско, С. Г.

doi:10.1007/s11094-017-1669-1

Cited by 18 publications

(5 citation statements)

References 3 publications

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“…1). Для животных интактной группы характерно практически полное отсутствие различий в размере правой и левой задних лап [20]. Из референтных препаратов наиболее выраженную антиэкссудативную активность через 24 ч после введения раствора формалина продемонстрировал индометацин, однако на 48-часовой отметке эксперимента разница в толщине лап крыс увеличивалась (табл.…”

Section: результатыunclassified

Study of the anti-exudative activity of new 3-cyano-1,4- dihydropyridines, cyanotioacetamide derivatives, on the model of acute formalin edema

Bochev,

Bibik,

Krivokolysko

et al. 2024

Sibirskij nauchnyj medicinskij zhurnal

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The inflammatory process accompanies most of the pathologies and requires pharmacological correction. In spite of significant achievements of scientists in the field of medicine and pharmacology, existing steroid and nonsteroidal antiinflammatory drugs have a number of undesirable reactions. To date, one of the most urgent directions is the search for new effective and safe drugs with anti-inflammatory activity. The aim of the study was to investigate the anti-exudative properties of new 3-cyano-1,4-dihydropyridines, cyanothioacetamide derivatives in the classical test of acute formalin edema. Material and methods. The study was conducted on 88 white rats weighing 210–250 g. The effectiveness of compounds was determined in a model of acute formalin edema, which was induced by subplantar injection of 0.1 ml of 2 % formalin solution into the right hind limb of the animals. The severity of exudation was evaluated oncometrically in comparison with reference drugs – ibuprofen, indomethacin, meloxicam and metamizole sodium. The studied substances were administered intragastrically at a dose of 5 mg/kg 1.5 hours before the induction of inflammation. Results. It was found that some compounds exhibit anti-exudative activity, more pronounced or similar to the activity of reference drugs. The laboratory sample with code mar-137 was the leading sample and outperformed the comparators; 24 hours after the modeling of edema, it exceeded ibuprofen (by 2.39 %), metamizole sodium (by 4.77 %) in anti-exudative efficacy and had an anti-inflammatory effect similar to the activity of indomethacin and meloxicam. Conclusions. Newly synthesized laboratory samples of 3-cyano-1,4-dihydropyridines, cyanothioacetamide derivatives, were found to exhibit pronounced anti-exudative activity and are of interest for further research as a new class of anti-inflammatory drugs.

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Section: результатыunclassified

Study of the anti-exudative activity of new 3-cyano-1,4- dihydropyridines, cyanotioacetamide derivatives, on the model of acute formalin edema

Bochev,

Bibik,

Krivokolysko

et al. 2024

Sibirskij nauchnyj medicinskij zhurnal

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“…Many of the compounds obtained in this way exhibit valuable practical properties. In particular, pyrido [2,1-b]- [1,3,5]thiadiazine derivatives 3 (Scheme 2) show high activity against tick-borne encephalitis virus and Powassan virus [41], exhibit a pronounced antiinfl ammatory effect [42], analeptic [43] and adaptogenic effect [44]. Disulfi des 4 (Hlg = F, Br) have moderate anti-HIV activity [45], compounds 5 and 6 are inhibitors of autotaxin [46], while hexahydroquinoline 7 inhibits betaamyloid peptide formation [47], which is considered one of the main factors in the development of the Alzheimer's disease.…”

Section: Doi: 101134/s107036322102002xmentioning

confidence: 99%

Synthesis and Analgesic Activity of New Heterocyclic Cyanothioacetamide Derivatives

Bibik

Dotsenko

et al. 2021

Russ J Gen Chem

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The reaction of cyanothioacetamide with aromatic aldehydes and 1,3-dicarbonyl compounds followed by aminomethylation or S-alkylation gave a series of heterocyclic derivatives with a 1,2,3,4-tetrahydropyridine or 1,4,5,6,7,8-hexahydroquinoline fragment. The resulting compounds were tested for analgesic activity in vivo. Some of the prepared compounds showed an antinociceptive effect superior to that of ketorolac in dynamics.

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“…Compounds III-IV ( Fig. 1) showed the best results, exceeding the sodium diclofenac 3.5 and 2.13 times, respectively (Bybik et al 2016).…”

Section: Introductionmentioning

confidence: 96%

“…The screening studies of the new tetrahydropyrido [2,1-b] [1,3,5] thiadiazine derivatives (Dotsenko et al 2014, Osolodkin et al 2013 showed that compounds I, II have the most evident analgesic activity. A number of substances showed a high analgesic activity, exceeding that of analgin (Bybik et al 2016). In addition, on the "formalin paw edema" model, the compounds with evident anti-inflammatory activity were found among the test samples.…”

Section: Introductionmentioning

confidence: 99%

The effect of derivatives of tetrahydropyrido[2,1-b][1,3,5] thiadiazine on hematologic indices of rats with subacute parotitis

Bibik¹,

Yaroshevskaya²,

Деменко³

et al. 2018

RRP

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Introduction: Regardless of belonging of NSAIDs to one or another chemical group, they all have common side effects that can occur when using these drugs for a long or short period. One type of toxicity in the spectrum of side effects of modern non-steroidal anti-inflammatory drugs is hematotoxicity. Objectives: to study the indices characterizing the red and white hematopoiesis in a clinical blood examination in animals with a simulated inflammation process against a background of pharmacocorrection with original thiadiazine derivatives. Methods: The experiments were carried out on 48 white pedigree mature rats of both sexes weighing 170–210 g. The tetrahydropyrido [2,1-b] [1,3,5] thiadiazine derivatives II, III and V were selected, since they showed the strongest anti-inflammatory, analgesic and antipyretic properties in the previous experiments. The animals were divided into eight groups: intact (rats without the pathology), control (with inlammation), referent 1 (inflammation+diclofenac sodium 0.5 mg/kg), referent 2 (inflammation+analgin 5 mg/kg), referent 3 (inflammation+indomethacin 5 mg / kg) and three test groups (with test substances administered at a dose of 5 mg/kg). Administration of the drugs was carried out for 14 days at the above doses. The standard methods were used to determine the number of erythrocytes, hemoglobin, color index, ESR, leukocytes and neutrophils. Results: In the analysis of the numerical results of the experiment, the valid ranges of values were determined for most parameters under study, which made it possible to use nonparametric statistical methods, including the Wilcoxon signed-rank test, to evaluate the reliability of differences. The use of tetrahydropyrido [2,1-b] [1,3,5] thiadiazine derivatives II, III, V in animals with experimental parotitis was accompanied by an increase in the number of erythrocytes in comparison with that in the control group. Conclusion: The studies of three derivatives of tetrahydropyrido [2.1-b] [1.3.5] thiadiazine, which have a high anti-inflammatory activity, proved that the compounds III and V have no hematotoxicity.

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Search for Anti-Inflammatory Agents in the Tetrahydropyrido[2,1-B ][1,3,5]-Thiadiazine Series

Cited by 18 publications

References 3 publications

Study of the anti-exudative activity of new 3-cyano-1,4- dihydropyridines, cyanotioacetamide derivatives, on the model of acute formalin edema

Study of the anti-exudative activity of new 3-cyano-1,4- dihydropyridines, cyanotioacetamide derivatives, on the model of acute formalin edema

Synthesis and Analgesic Activity of New Heterocyclic Cyanothioacetamide Derivatives

The effect of derivatives of tetrahydropyrido[2,1-b][1,3,5] thiadiazine on hematologic indices of rats with subacute parotitis

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