ChemInform Abstract: Synthesis and Sedative Activity of D,L‐Tetrahydropalmatine.

Виноградова, В. И.; Yunosov, M. S.; Rezhepov, Zh.; Sadritdinov, F

doi:10.1002/chin.198323254

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“…The obtained data are consistent with the previous studies (Spasov et al 2018) on the combination of benzodiazepine and benzimidazole scaffolds, which also resulted in obtaining the compounds -diazepino[1,2-a]benzimidazoles -with a pronounced neurotropic activity due to the native diazepine fragment, and mitigated undesirable effects due to the presence of the benzimidazole group. According to the data, the acute toxicity of diazepam when administered orally to the mice is 48 mg/kg (Vinogradova et al 1983). For 1,2,4-triazole derivatives, the LD 50 is at the level of 1250-2000 mg/kg, which makes it possible to classify this class of compounds as low-toxic (Ovsyannikova et al 2017).…”

Section: Resultsmentioning

confidence: 99%

Screening of anxiolytic properties and analysis of structure-activity relationship of new derivatives of 6-(4-methoxy)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD

Skripka¹,

Spasov²,

Maltsev³

et al. 2021

RRP

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Introduction: Searching for new compounds with anti-anxiety activity resulting from the combination of privileged scaffolds is a promising direction in medicinal chemistry and in the development of new drugs. Anxiolytic potential and cytotoxic properties of previously synthesized molecules, containing fragments of 2,3-benzodiazepine and 1,2,4-triazole – 6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-A][2,3]benzodiazepines under the generic code RD were studied. Materials and methods: Screening for anxiolytic activity was performed on elevated plus maze (EPM) and open field (OF) test models. Structural and functional analysis of the anti-anxiety activity of the studied substances was carried out. A degree of muscle relaxant effect of the substances was assessed in the tests Grid, Wire, and Rotarod. A cytotoxicity study of RD compounds was carried out using an MTT assay on human hepatocellular carcinoma cells HepG2. Results and discussion: For a number of novel triazolo[3,4-a][2,3]benzodiazepine derivatives, a prominent anxiolytic activity was manifested in terms of EPM test. The results of OF test were consistent with the obtained data and confirmed the presence of the sought activity in the leading compounds. There was no significant effect on muscle tone for the compounds under study. It was observed that RD compounds possessed no cytotoxic properties and were safe for further studies in vivo. Conclusion: Among the new derivatives of 6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD, substances (RD-4, 12, 13) with a high anxiolytic activity comparable to diazepam and tofisopam were found. The most promising compound is RD-4 due to its pronounced anxiolytic and low cytotoxic properties.

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Section: Resultsmentioning

confidence: 99%

Screening of anxiolytic properties and analysis of structure-activity relationship of new derivatives of 6-(4-methoxy)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD

Skripka¹,

Spasov²,

Maltsev³

et al. 2021

RRP

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ChemInform Abstract: Synthesis and Sedative Activity of D,L‐Tetrahydropalmatine.

Abstract: D,L‐Tetrahydro‐palmatin (IV) wird aus Homoveratrylamin (I) und dem Isochromanon(II) über (III) hergestellt.

Cited by 1 publication

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Screening of anxiolytic properties and analysis of structure-activity relationship of new derivatives of 6-(4-methoxy)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD

Screening of anxiolytic properties and analysis of structure-activity relationship of new derivatives of 6-(4-methoxy)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD

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