A previous study was conducted on the synthesis and antibacterial evaluation of Mannich bases of 2-(thioalkyl)-1H-methylbenzimidazole derivatives. The results of this study showed that certain 2-(thioalkyl)-1H-methylb...A previous study was conducted on the synthesis and antibacterial evaluation of Mannich bases of 2-(thioalkyl)-1H-methylbenzimidazole derivatives. The results of this study showed that certain 2-(thioalkyl)-1H-methylbenzimidazole and 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl)benzimidazole derivatives possess antibacterial activities against clinical strains, such as Escherichia coli, Klebsiella pneumonia (Gram-negative bacteria), Staphylococcus aureus and Pseudomonas aeruginosa (Gram-positive bacteria). Following these favorable results, we extended the antibacterial evaluation of this series of molecules to environmental strains. The aim of this study was to assess the impact of the methyl-piperidine group fixed at position-1 of this new series of benzimidazoles on the antibacterial activity of environmental strains. In addition, we first evaluated the antibacterial activity of four 2-(thioalkyl)methylbenzimidazole derivatives and then that of five 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives. This study allowed us to show that compounds 1d and 1e could inhibit bacterial growth in vitro of the Enterobacteria P1 strain with inhibition diameters of 17.3 ± 0.6 mm and 10 ± 0.0 mm, respectively. However, addition of methyl-piperidinyl in this series showed that five (5) of 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives had an inhibitory effect on the in vitro growth of bacterial strains used except on Enterobacteria P2 with inhibition diameters between 10.0 ± 0.8 mm and 27.9 ± 1.4 mm. The introduction of the methyl-piperidinyl group at the 1-position of 2-(thioalkyl)-1H-methylbenzimidazole derivatives greatly improved the antibacterial activity against environmental bacteria such as Escherichia coli A1, A2, A3, and A4 and two Enterobacteria P1.展开更多
During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of produc...During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of product IM is postulated and discussed on the basis of deuterium labelling.展开更多
In this study,we aimed to determine the radiation parameters of some potential bioactive compounds.1-Aryl-3-dibenzylamino-propane-1-on hydrochloride type Mannich bases were synthesized via classical conventional heati...In this study,we aimed to determine the radiation parameters of some potential bioactive compounds.1-Aryl-3-dibenzylamino-propane-1-on hydrochloride type Mannich bases were synthesized via classical conventional heating method.Aryl part was changed as phenyl(C6H5),4-methylphenyl(4-CH3C6H4),4-fluorophenyl(4-FC6H4),4-nitrophenyl(4-NO2C6H4),4-chlorophenyl(4-ClC6H4),4-bromophenyl(4-BrC6H4),and 2-thienyl(C4H3S-2-yl).Mass attenuation coefficient(μm),effective atomic number(Zeff)and effective electron density(Nel)of compounds were determined experimentally and theoretically for at 8.040,8.910,13.40,14.96,17.48,19.61,22.16,24.94,32.19,36.38,44.48,50.38and 59.54keV photon energies by using an HPGe detector with a resolution of 182eV at 5.9keV.Radiation parameters of these compounds which can be anti-cancer drug candidate were given in the tables.The results show that phenyl ring behave like thiophene ring in terms of radiation absorption.It is thought that the results of study may drive allow the development of drug candidate new compounds in medical oncology.展开更多
We have synthesized mannich base cyclohexanone using microwave irradiation method,and studied their pharma-cological activity.Based on analytical and spectral(IR,NMR and Mass) data,a number of mono as well as double m...We have synthesized mannich base cyclohexanone using microwave irradiation method,and studied their pharma-cological activity.Based on analytical and spectral(IR,NMR and Mass) data,a number of mono as well as double mannich base cyclohexanones have been synthesized from primary and secondary amines and formaldehyde,and then purified and characterized. The required 3-aryl-2,4-diacetyl-5-hydroxy-5-methylcyclohexanone was prepared from appropriate aldehyde and acetylacetone. The synthesized compounds were screened for analgesic activity via standard approaches,and they have shown positive analgesic activity.展开更多
文摘A previous study was conducted on the synthesis and antibacterial evaluation of Mannich bases of 2-(thioalkyl)-1H-methylbenzimidazole derivatives. The results of this study showed that certain 2-(thioalkyl)-1H-methylbenzimidazole and 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl)benzimidazole derivatives possess antibacterial activities against clinical strains, such as Escherichia coli, Klebsiella pneumonia (Gram-negative bacteria), Staphylococcus aureus and Pseudomonas aeruginosa (Gram-positive bacteria). Following these favorable results, we extended the antibacterial evaluation of this series of molecules to environmental strains. The aim of this study was to assess the impact of the methyl-piperidine group fixed at position-1 of this new series of benzimidazoles on the antibacterial activity of environmental strains. In addition, we first evaluated the antibacterial activity of four 2-(thioalkyl)methylbenzimidazole derivatives and then that of five 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives. This study allowed us to show that compounds 1d and 1e could inhibit bacterial growth in vitro of the Enterobacteria P1 strain with inhibition diameters of 17.3 ± 0.6 mm and 10 ± 0.0 mm, respectively. However, addition of methyl-piperidinyl in this series showed that five (5) of 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives had an inhibitory effect on the in vitro growth of bacterial strains used except on Enterobacteria P2 with inhibition diameters between 10.0 ± 0.8 mm and 27.9 ± 1.4 mm. The introduction of the methyl-piperidinyl group at the 1-position of 2-(thioalkyl)-1H-methylbenzimidazole derivatives greatly improved the antibacterial activity against environmental bacteria such as Escherichia coli A1, A2, A3, and A4 and two Enterobacteria P1.
基金the National Natural Science Foundation of China.
文摘During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of product IM is postulated and discussed on the basis of deuterium labelling.
文摘In this study,we aimed to determine the radiation parameters of some potential bioactive compounds.1-Aryl-3-dibenzylamino-propane-1-on hydrochloride type Mannich bases were synthesized via classical conventional heating method.Aryl part was changed as phenyl(C6H5),4-methylphenyl(4-CH3C6H4),4-fluorophenyl(4-FC6H4),4-nitrophenyl(4-NO2C6H4),4-chlorophenyl(4-ClC6H4),4-bromophenyl(4-BrC6H4),and 2-thienyl(C4H3S-2-yl).Mass attenuation coefficient(μm),effective atomic number(Zeff)and effective electron density(Nel)of compounds were determined experimentally and theoretically for at 8.040,8.910,13.40,14.96,17.48,19.61,22.16,24.94,32.19,36.38,44.48,50.38and 59.54keV photon energies by using an HPGe detector with a resolution of 182eV at 5.9keV.Radiation parameters of these compounds which can be anti-cancer drug candidate were given in the tables.The results show that phenyl ring behave like thiophene ring in terms of radiation absorption.It is thought that the results of study may drive allow the development of drug candidate new compounds in medical oncology.
文摘We have synthesized mannich base cyclohexanone using microwave irradiation method,and studied their pharma-cological activity.Based on analytical and spectral(IR,NMR and Mass) data,a number of mono as well as double mannich base cyclohexanones have been synthesized from primary and secondary amines and formaldehyde,and then purified and characterized. The required 3-aryl-2,4-diacetyl-5-hydroxy-5-methylcyclohexanone was prepared from appropriate aldehyde and acetylacetone. The synthesized compounds were screened for analgesic activity via standard approaches,and they have shown positive analgesic activity.
