- Effect of optimized structure and electronic properties of some benzimidazole derivatives on corrosion inhibition of mild steel in hydrochloric acid medium: Electrochemical and theoretical studies
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Abstract The corrosion inhibitive action of a few benzimidazole derivatives namely 2-(benzamido) ethylbenzimidazole (BAEBI), 2-(β-benzenesulphonamido) ethylbenzimidazole (BSAEBI), 2-(benzamido) methylbenzimidazole (BAMBI) and 2-(β-benzenesulphonamido) met
- Dutta, Alokdut,Panja, Sujit Sankar,Nandi,Sukul, Dipankar
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p. 921 - 929
(2015/08/06)
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- Design, synthesis, and enzyme kinetics of novel benzimidazole and quinoxaline derivatives as methionine synthase inhibitors
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Methionine synthase catalyzes the transfer of a methyl group from 5-methyltetrahydrofolate to homocysteine, producing methionine and tetrahydrofolate. Benzimidazole and deazatetrahydrofolates derivatives have been shown to inhibit methionine synthase by competing with the substrate 5-methyltetrahydrofolate. In this study, a novel series of substituted benzimidazoles and quinoxalines were designed and assessed for inhibitory activity against purified rat liver methionine synthase using a radiometric enzyme assay. Compounds 3g, 3j, and 5c showed the highest activity against methionine synthase (IC50: 20 μM, 18 μM, 9 μM, respectively). Kinetic analysis of these compounds using Lineweaver-Burk plots revealed characteristics of mixed inhibition for 3g and 5c; and uncompetitive inhibition for 3j. Docking study into a homology model of the rat methionine synthase gave insights into the molecular determinants of the activity of this class of compounds. The identification of these drug-like inhibitors could lead the design of the next generation modulators of methionine synthase.
- Elshihawy, Hosam,Helal, Mohamed A.,Said, Mohamed,Hammad, Mohamed A.
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p. 550 - 558
(2014/01/17)
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- Reaction of o-Phenylenediamine with 2-Oxazolin-5-ones
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The reaction of o-phenylenediamine (2) with 2-oxazolin-5-ones (1a-c) gives benzimidazoles (4a-c) in the presence of gl. acetic acid.The intermediates 3a,b can be isolated only under neutral conditions. 4-(o-Aminoanilinomethylene)-2-phenyl-2-oxazolin-5-one (5) is formed, on heating 1d with 2, which is resistant to ring expansion.
- Tikdari, Ahmad M.,Mukerjee, Arya K.
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- Studies on Potential Antibacterial and Chelating Agents: Part I - Synthesis, Physicochemical Properties and Antibacterial Screening of Some Benzimidazoles
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Six properly substituted benzimidazoles (I-VI) suitable for chelation have been synthesised from benzoylamino acids by condensation with o-phenylenediamine following Phillips and fusion methods.Dissociation constants of the benzoyl derivatives of glycine, (dl)-α-alanine, β-alanine, L-(-)-aspartic acid, L-(+)-glutamic acid and the six protonated benzamidobenzimidazoles (I-VI) in water-dioxane (1:1) at constant ionic strength (μ=0.5) at 20 deg C +/- 0.1 deg C have been determined by potentiometric titration.Structures of I-VI have been established on the basis of their elemental analysis, synthetic route, IR and PMR spectra and pK* values.Some of the compounds show significant antibacterial activity against gram + ve organisms only whereas corresponding sulphonamidobenzimidazoles are active against the gram - ve organism E. coli.
- Nandi, M. M.,Ray, Ruma
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p. 222 - 224
(2007/10/02)
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