Synthesis and antimicrobial activity of 4-substituted thiazol-2-yl hydrazine derivatives of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carbaldehyde

The manuscript reports synthesis and antimicrobial activity of several novel heterocyclic compounds in which 1,4-disubstituted 1,2,3-triazole synthesized via click chemistry approach and 4-aryl (5a-h) and 4-piperazinyl amide (7a-e) or 4-aryl amide (8a-e) substituted thiazole rings, are bridged through hydrazine linkage. Structures of all the synthesized compounds have been elucidated using 1H and 13C NMR and mass spectral analysis. In vitro antimicrobial screening of the target compounds has been carried out against six bacterial species viz. E. coli, P. aeruginosa, B. subtilis, S. pyogenes, K. pneumoniae and S. aureus and four fungal species viz. C. albicans, T. viride, A. flavus and A. brasiliensis. The activity study revealed that many of the compounds possess moderate to good activity against the tested microorganisms. The active compounds have been further studied to determine the minimum inhibitory concentration (MIC)

Synthesis and antimicrobial activity of 4-substituted thiazol-2-yl hydrazine derivatives of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carbaldehyde

716-723The manuscript reports synthesis and antimicrobial activity of several novel heterocyclic compounds in which 1,4-disubstituted 1,2,3-triazole synthesized via click chemistry approach and 4-aryl (5a-h) and 4-piperazinyl amide (7a-e) or 4-aryl amide (8a-e) substituted thiazole rings, are bridged through hydrazine linkage. Structures of all the synthesized compounds have been elucidated using 1H and 13C NMR and mass spectral analysis. In vitro antimicrobial screening of the target compounds has been carried out against six bacterial species viz. E. coli, P. aeruginosa, B. subtilis, S. pyogenes, K. pneumoniae and S. aureus and four fungal species viz. C. albicans, T. viride, A. flavus and A. brasiliensis. The activity study revealed that many of the compounds possess moderate to good activity against the tested microorganisms. The active compounds have been further studied to determine the minimum inhibitory concentration (MIC)

An efficient total synthesis of (±)-pregabalin

631-634The synthesis of (±)-pregabalin has been accomplished by oxidation and reduction of 2-benzyl-4-methyl pentanenitrile. The synthetic strategy involves ruthenium chloride catalyzed oxidation of the phenyl ring into carboxylic acid and reduction of nitrile into amine using sodium borohydride and nickel chloride. The approach delineated here is notable for its simplicity and efficient synthesis

A simple and efficient approach to the synthesis of 2-substituted benzimidazole via sp3 C–H functionalization

A facile and novel approach to the synthesis of 2-substituted benzimidazole was developed via a tandem reaction following sp3 C–H functionalization. Here we report a simple, efficient and tandem oxidative dehydrative coupling reaction of N-benzylbezene-1,2-diamine in the presence of oxidant tert-butyl hydroperoxide (TBHP) in solvent acetonitrile to give substituted benzimidazole

Synthesis and biological activity of novel derivatives of 2-(5-(3-fluro-4-methoxy phenyl)-1H-pyrazol-3-yl)-5-aryl-1,3,4-oxadiazole

892-897A series of new 1,3,4-oxadiazole derivatives have been synthesized by condensation of 5-(3-fluro-4-methoxyphenyl)-1H-pyrazole-3-carbohydrazide with different substituted benzoic acids. All the synthesized compounds have been screened for antibacterial activity against S. aureus, E. coli, B. subtilis, P. aeruginosa, S. pyogenes, K. terrigena, K. Pneumoniae and antifungal activity against T. viride, A. flavus, A. brasillansis and C. albicans. Most of the synthesized compounds show good antimicrobial activity

Synthesis and biological evaluation of a series of 1,4-disubstituted 1,2,3-triazole derivatives as possible antimicrobial agents

Three series of novel compounds derived from 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid bearing piperazine carboxamides, (5-(substituted phenyl)-1,3,4-oxadiazol-2-yl) and (5-(alkylthio)-1,3,4-oxadiazol-2-yl) substitutions at the 4-position were synthesized. Synthesized compounds were characterized by 1H NMR, 13C NMR and mass spectral analysis and evaluated for their antimicrobial activities. Interestingly, most of the compounds exhibit moderate to good activities against tested Gram-positive, Gram-negative bacterial strains as well as fungal strains

Synthesis and biological screening of novel pyrazole and isoxazole derivatives

979-987Novel 1,5-disubstituted pyrazole and isoxazole derivatives like, aryl<span style="mso-bidi-font-weight:bold;mso-bidi-font-style: italic"> 5-(3-fluoro-4-methoxyphenyl)-1H-pyrazole-3-carboxylic acid 8a-e, [(aryl)-piperazin-1-yl]-[5-(3-fluoro-4-methoxyphenyl)-isoxazol-3-yl]-methanone 9a-e, aryl <span style="mso-bidi-font-weight: bold;mso-bidi-font-style:italic">5-(3-fluoro- 4-methoxyphenyl)-1H-pyrazole-3-carboxylic acid 10a-e have been synthesized and characterized using IR, 1H NMR, 13C NMR and mass spectral analysis. All the synthesized compounds have been screened for their antibacterial activity against <span style="mso-ansi-language: PT-BR" lang="PT-BR">S. aureus, E. coli, <span style="mso-ansi-language: PT-BR" lang="PT-BR">B. subtilis, P. aeruginosa, <span style="mso-ansi-language: PT-BR" lang="PT-BR">S. pyogenes, K. terrigena <span style="mso-ansi-language: PT-BR" lang="PT-BR">and K. pneumoniae and antifungal activity against T. viride, A. flavus, A. brasillansis, and C. albicans. Interestingly all the synthesized compounds exhibit good antibacterial and antifungal activity. </span

Synthesis and antimicrobial activity of new S-alkyl isothiosemicarbazone derivatives of pyrimidine

565-569A series of S-alkyl isothiosemicarbazone derivatives of 2,4,6-trisubstituted pyrimidine have been synthesized. All the synthe-sized compounds are characterized by IR, NMR and mass spectro-metry. Most of the synthesized compounds show significant antibacterial and antifungal activity against the tested microorganisms