ChemInform Abstract: Synthesis and Pharmacological Activity of Some 2,3‐Dihydroimidazo‐(1,2‐a)benzimidazoles and Their Intermediates.

Анисимова, В. А.; Levchenko, M. V.; Kovalev, G. V.; Спасов, А. А.; Дудченко, Г. П.; Antonyan, S. G.; Bessudnova, N. V.; Libinzon, R.E.

doi:10.1002/chin.198744191

Cited by 3 publications

(4 citation statements)

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“…The synthesis of novel 2-aminobenzimidazole (AmBI) [13,14] derivatives and fused benzimidazole derivatives was carried out, including N 9 -imidazo [1,2-a] benzimidazoles (N 9 -ImBI) [15][16][17], N 1 -imidazo[1,2-a]benzimidazoles (N 1 -ImBI) [18,19], N 9 -2,3-dihydroimidazo[1,2-a]benzimidazoles (N 9 -DhImBI) [20,21], N 1 -2,3-dihydroimidazo[1,2-a]benzimidazoles (N 1 -DhImBI) [18,19], and 2,3,4,10-tetrahydropyrimido[1,2-a]benzimidazoles (PrmBI) [22][23][24].…”

Section: Resultsmentioning

confidence: 99%

“…Synthesis of 9-diethylaminoethyl-2,3-dihydroimidazo[1,2-a]benzimidazole dihydrochloride (RU-254, diabenol) is readily realized through condensation of 2-amino-1-diethylaminoethylbenzimidazole with an excess of dibromoethane and subsequent transformation of the resulting of 9-diethylaminoethyl-2,3-dihydroimidazo[1,2-a]benzimidazole dihydrobromide to the base and the desired dihydrochloride [21].…”

Section: Synthesismentioning

confidence: 99%

See 1 more Smart Citation

Antidiabetogenic Features of Benzimidazoles

Спасов¹,

Vassiliev²,

Анисимова³

et al. 2019

Chemistry and Applications of Benzimidazole and Its Derivatives

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Literature data on the insulinogenic effect of 2-aminobenzimidazole prompted us to investigate its novel derivatives, particularly those containing an additional fused cycle in C1,2-α position, including imidazole, dihydroimidazole, or tetrahydropyrimidine ring. Consensus analysis of the hypoglycemic effect of these compounds performed with IT Microcosm and PASS system revealed that activity is mostly characteristic for N 9 -2,3-dihydroimidazo[1,2-a]benzimidazole derivatives. Substructural analysis of hypoglycemic activity identified substituents that determine the greatest pharmacological effect. According to the in silico assessment of the ADME properties, RU-254 was nominated as a lead compound due to the most optimal calculated and experimental activity and pharmacokinetic parameters. Preclinical studies have shown that identified compound has a pronounced insulinogenic effect and hypoglycemic effect, both in intact animals and in animals with experimental diabetes mellitus. RU-254 also reduces the level of glycated hemoglobin upon chronic administration, slightly decreases the activity of DPP-4, and increases the average number of Langerhans islets in the pancreas. Pharmaceutical drug formulation of RU-254 was developed and investigated for pharmacokinetic, pharmacodynamic, and toxicological properties. The dosage form of the drug under the name limiglidol (compound RU-254, diabenol) was evaluated in the full cycle of clinical studies that confirmed the safety, tolerability, and prominent antidiabetic properties of the drug.

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Section: Resultsmentioning

confidence: 99%

Section: Synthesismentioning

confidence: 99%

Antidiabetogenic Features of Benzimidazoles

Спасов¹,

Vassiliev²,

Анисимова³

et al. 2019

Chemistry and Applications of Benzimidazole and Its Derivatives

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show abstract

“…Transition metal complexes containing imidazole and their derivatives have been shown to possess pharmacological activity [1,2] and have been used as antitumor and antimicrobial agents. Nitrogen heterocycles in general, and benzimidazole and their derivatives in particular, have been investigated for their antitumor, antibacterial, anti fungicidal, anticarcinogenic, anti-tubercular, anti-allergic and poliovirus inhibitor properties.…”

Section: Introductionmentioning

confidence: 99%

Molecular Structure of Metal Complexes of Certain Benzimidazole Derivatives

Manjunatha¹

2018

OMCIJ

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“…As shown in [1], 1-allyl-3-alkyl-(arylalkyl, dialkylaminoalkyl)-2-imino-2,3-dihydro-1H-benzimidazoles take up hydrogen bromide at the allyl group, and next follows heterocyclization with formation of 9-substituted 2-methyl-2,3-dihydroimidazo [1,2-a]benzimidazoles. Some cyclization products exhibited interesting biological properties [6]. In continuation of these studies, we synthesized 1-allyl-2-aminobenzimidazoles containing an acylmethyl group in the 3-position.…”

mentioning

confidence: 99%