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Synthesis and antimycobacterial activity of benzimidazole derivatives

Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives.

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Synthesis of benzimidazole derivatives as potential ..

We have designed and synthesized a series of novel 2-substituted benzimidazole and pyrimidine derivatives via the cyclization reaction of protected amino acids with O-phenylendiamine and 1,8-naphtalendiamine. All synthesized compounds were confirmed by FT-IR, 1H NMR and 13C-NMR and elemental analysis. Also the synthetic compounds were screened for their inhibitory effect on yeast and rat intestinal α-glucosidases and compounds 4c, 4d, 5c and 5d displayed significant ability on inhibition of the enzymes. Therefore, these compounds, open new avenues for the development of anti-hyperglycemic therapeutics agents to the treatment of type 2 diabetes.

A series of new benzimidazole derivatives were synthesized by the solid-state condensation ..
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The synthesis and comprehensive characterization of the excited states of four novel triphenylamine–benzimidazole derivatives has been undertaken in solution (ethanol and methylcyclohexane) at room temperature. This includes the determination of the absorption, fluorescence, and triplet–triplet absorption spectra, together with quantum yields of fluorescence, internal conversion, intersystem crossing, and singlet oxygen. From the overall data the radiative and radiationless rate constants could be obtained, and it is shown that the compounds are highly emissive with the radiative decay dominating, with more than 70% of the quanta loss through this deactivation channel. The basic structure of the triphenylamine–benzimidazole derivatives (1a) was modified at position 5 of the heterocyclic moiety with electron-donating (OH (1b), OCH3 (1c)) or electron-withdrawing groups (CN, (1d)). It was found that the photophysical properties remain basically unchanged with the different substitutions, although a marked Stokes shift was observed with 1d. The presence and nature of a charge-transfer transition is discussed with the help of theoretical (DFT and TDFT) data. All compounds displayed exceptionally high thermal stability (between 399 and 454 °C) as seen by thermogravimetric analysis.

Synthesis of some novel benzimidazole derivatives and …

and , “Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives” Journal of the Korean Chemical Society, 6.
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In the light of above observations, we have recently performed some study including the synthesis of some benzimidazole and pyrimidine derivatives (,). Results of these investigations have persuaded us to apply some structural modifications to progress their biological activities. So, we have designed some synthesis strategies that include the synthesis of benzimidazole and pyrimidine systems containing protected amino acids. To date there are no reports available describing synthesis and α-glucosidase inhibition activities of these classes of heterocycles. Phosphorus oxychloride was necessary for this condensation, which activate the carboxyl group of amino acids and increases its electrophilicity to enhance the addition of diamine.

In the first step, amino acids were chosen as starting material. Phthalic anhydride was reacted with amino acids to protect the amino group of them and converted to N-phthaloyl-L-amino acids (). Secondly, to synthesis the benzimidazole and pyrimidine derivatives, N-phthaloyl-L-amino acids were reacted with O-phenylendiamine or 1,8-naphtalendiamine respectively in POCl3. Synthetic pathway of the compounds is given in and .

Synthesis and Evaluation of Selected Benzimidazole Derivatives as ..

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Over the past years, several benzimidazole and pyrimidine derivatives have been synthesized and widely screened for their biological activities. These classes of hetrocycles have found applications in diverse pharmacological areas such as antibacterial, antibiotics (,), anticancer (), anti-inflammatory (), antifungal (), antidiabetic (), enzyme inhibitors (,), anti-hepatitis C (), cytotoxicity () and antihypertensive (). More over these derivatives were applied as antiparasitic, elastase inhibitors, anti-stress, antioxidant, antiviral (anti-HIV), anticonvulsant and antiprotozoal (-). Because of this wide range of biological and pharmaceutical activities and industrial applications, benzimidazole and pyrimidine moieties have received much attention in developing new therapeutic agents. Several methods are available for the benzimidazole synthesis. The more attractive method of benzimidazoles synthesis involves cyclocondensation of an aldehyde with substituted 1,2-phenylenediamines in the presence of an acidic catalyst as dehydrating agent. Pyrimidine derivatives were synthesized by different procedures such as biginelli reaction and the other multi component reactions (-). In addition this structure was synthesized by the reaction of 1,8-naphtalendiamine with an aldehyde in the presence of an acidic catalyst ().

22.05.2012 · Synthesis of novel benzimidazole derivatives: as potent analgesic agent
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