Synthesis and Pharmacological Activity of 1‐ and 10‐N‐Substituted 1(10),2,3,4‐Tetrahydropyrimido[1,2‐a]benzimidazoles.

Анисимова, В. А.; Osipova, M. M.; Спасов, А. А.; Turchaeva, A. F.; Дудченко, Г. П.; Larionov, N. P.; Kovalev, S. G.

doi:10.1002/chin.200304154

Cited by 4 publications

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“…It has been suggested that hyperinsulinemia may have increase free radicals and therefore promote aging, independent of glycemia [39,77,78,151,152]. Plasma levels of lipid hydroperoxides are higher, and antioxidant factors are lower in individuals who are resistant to insulin-stimulated glucose disposal but otherwise glucose tolerant, nonobese, and normotensive [77].…”

Section: Introductionmentioning

confidence: 99%

Metformin for aging and cancer prevention

Anisimov

2010

Aging

133

102

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Studies in mammals have led to the suggestion that hyperglycemia and hyperinsulinemia are important factors in aging. Insulin/insulin-like growth factor 1 (IGF-1) signaling molecules that have been linked to longevity include daf-2 and InR and their homologues in mammals, and inactivation of the corresponding genes increases life span in nematodes, fruit flies and mice. It is possible that the life-prolonging effect of caloric restriction is due to decreasing IGF-1 levels. Evidence has emerged that antidiabetic drugs are promising candidates for both life span extension and prevention of cancer. Thus, antidiabetic drugs postpone spontaneous carcinogenesis in mice and rats, as well as chemical and radiation carcinogenesis in mice, rats and hamsters. Furthermore metformin seems to decrease cancer risk in diabetic patients.

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Section: Introductionmentioning

confidence: 99%

Metformin for aging and cancer prevention

Anisimov

2010

Aging

133

102

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“…A total of 27 new compounds were synthesized as described previously [6] , [7] , [8] , [9] , [10] , [11] and tested for IOP lowering effect in ocular normotensive rats. These compounds included twenty 9H-imidazo[1,2-a]benzimidazoles, four 10H-pyrimido[1,2-a]benzimidazoles, two 1H-pyrimido[1,2-a]benzimidazoles and one 1H-imidazo[1,2-a]benzimidazole.…”

Section: Experimental Design Materials and Methodsmentioning

confidence: 99%

“…Benzimidazoles are heterocyclic compounds that are known for numerous therapeutic effects and are recognized as important pharmacophore in drug discovery [1] , [2] , [3] , [4] , [5] , [6] , [7] , [8] , [9] , [10] , [11] , [12] . Over the past years, several benzimidazole derivatives have been synthesized and their pharmacological activities investigated.…”

Section: Datamentioning

confidence: 99%

“…This data is supplementary to [1] presenting the effects of benzimidazole-based compounds on IOP of ocular normotensive rats. These compounds included twenty 9H-imidazo[1,2-a]benzimidazoles, four 10H-pyrimido[1,2-a]benzimidazoles, two 1H-pyrimido[1,2-a]benzimidazoles and one 1H-imidazo[1,2-a]benzimidazole [6] , [7] , [8] , [9] , [10] , [11] . In present article, data combine the results of pharmacophore and neural network analysis.…”

Section: Datamentioning

confidence: 99%

“…A total of 27 new compounds were synthesized as described previously and tested for IOP lowering effect in rats. These compounds included twenty 9H-imidazo[1,2-a]benzimidazoles, four 10H-pyrimido[1,2-a]benzimidazoles, two 1H-pyrimido[1,2-a]benzimidazoles and one 1H-imidazo[1,2-a]benzimidazole [2] , [3] , [4] , [5] , [6] , [7] , [8] , [9] , [10] , [11] . Experimental features All compounds were topically applied as a single drop, unilaterally, at 3 different concentrations (0.1%, 0.2% and 0.4%).…”

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confidence: 99%

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Relationship between intraocular pressure lowering effect and chemical structure of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole derivatives

et al. 2018

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This article contains data that relate to the study carried out in the work of Marcus et al. (2018) [1]. Data represent an information about pharmacophore analysis of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole derivatives and results of construction of the relationship between intraocular pressure (IOP) lowering activity and hypotensive activity of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole derivatives using a multilayer perceptron artificial neural network. In particular, they include the ones listed in this article: 1) table of all pharmacophores of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole derivatives that showed IOP lowering activity; 2) table of all pharmacophores of the compounds that showed absence of IOP lowering activity; 3) table of initial data for artificial neural network analysis of relationship between IOP activity and hypotensive activity of this chemical series; 4) graphical representation of the best neural network model of this dependence; 5) original txt-file of results of pharmacophore analysis; 6) xls-file of initial data for neural network modeling; 7) original stw-file of results of neural network modeling; 8) original xml-file of the best neural network model of dependence between IOP lowering activity and hypotensive activity of these azole derivatives. The data may be useful for researchers interested in designing new drug substances and will contribute to understanding of the mechanisms of IOP lowering activity.

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Data on the effects of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds on intraocular pressure of ocular normotensive rats

et al. 2018

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This data is to document the intraocular pressure (IOP) lowering activity of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds in ocular normotensive rats. Effects of single drop application of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds on IOP in ocular normotensive rats are presented at 3 different concentrations (0.1%, 0.2% and 0.4%). Time course of changes in IOP is presented over 6 h period post-instillation. The IOP lowering activities of test compounds were determined by assessing maximum decrease in IOP from baseline and corresponding control, duration of IOP lowering and area under curve (AUC) of time versus response curve. Data shown here may serve as benchmarks for other researchers studying IOP-lowering effect of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds and would be useful in determining therapeutic potential of these test compounds as IOP lowering agents.

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Synthesis and Pharmacological Activity of 1‐ and 10‐N‐Substituted 1(10),2,3,4‐Tetrahydropyrimido[1,2‐a]benzimidazoles.

Cited by 4 publications

References 0 publications

Metformin for aging and cancer prevention

Metformin for aging and cancer prevention

Relationship between intraocular pressure lowering effect and chemical structure of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole derivatives

Data on the effects of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds on intraocular pressure of ocular normotensive rats

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