PTSA-catalyzed selective synthesis and antibacterial evaluation of 1,2-disubstituted benzimidazoles

Effective Synthesis and Anti‐Mycobacterial Activity of Isoxazole‐Substituted Piperazine Derivatives

“…Antibacterial Activity Assays: According to the literature, [53,54] Mycobacteria smegmatis MC 2 155 strain was selected as model organisms for the determination of the minimum inhibitory concentrations (MICs) of the synthesized compounds 1,4-bis((3arylisoxazol-5-yl)methyl)piperazines (6a-6l). The MIC was determined by the microdilution method.…”

p-Toluenesulfonic acid-promoted organic transformations for the generation of molecular complexity

“…A plausible mechanistic approach was proposed by the authors where p-TSA was believed to catalyse the initial protonation of nitrogen on morpholine unit followed by the successive addition of o-phenylenediamines/o-aminothiophenols and elimination of ethyl mercaptane through intramolecular cyclization to afford the corresponding products (Scheme 47). Another straightforward protocol for the synthesis of a range of 1,2-disubstituted benzimidazoles has been studied by Zhang and co-workers 72 in EtOH medium at 78 °C. p-Toluenesulfonic acid-promoted cyclocondensation of o-phenylenediamine and aldehydes gave the desired 1,2-disubstituted benzimidazoles in moderate to good yields within 30 min (Scheme 48).…”

“…Another straightforward protocol for the synthesis of a range of 1,2-disubstituted benzimidazoles has been studied by Zhang and co-workers 72 in EtOH medium at 78 °C. p -Toluenesulfonic acid-promoted cyclocondensation of o -phenylenediamine and aldehydes gave the desired 1,2-disubstituted benzimidazoles in moderate to good yields within 30 min (Scheme 48).…”

Na2S2O3 Catalyzed Three‐Component Synthesis and Anti‐Bacterial Activity of 3‐Methyl‐4‐(hetero)arylmethylene isoxazole‐5(4H)‐ones

“…According to the literature, [33,34] Mycobacteria smegmatis MC 2 155 strain was selected as model organisms for the determination of the minimum inhibitory concentrations (MICs) of the synthesized 3-methyl-4-(hetero) arylmethylene isoxazole-5(4H)-ones. Through measuring the growth of Mycobacteria smegmatis MC 2 155 at different concentrations of synthesized compounds, the MIC values of these 16 compounds were obtained by using rifampicin as a reference.…”