7147-66-2Relevant articles and documents
Bisbenzimidazole Derivatives as Potential Antimicrobial Agents: Design, Synthesis, Biological Evaluation and Pharmacophore Analysis
Ersan, Ronak Haj,Bolelli, Kayhan,Gonca, Serpil,Dogen, Aylin,Burmaoglu, Serdar,Algul, Oztekin
, p. 149 - 158 (2021/05/13)
In an attempt to design and synthesize a potent class of antimicrobials, 1,2-phenylenediamine derivatives were reacted with various aliphatic and heteroaliphatic dicarboxylic acids to generate a small library of 26 head-to-head bisbenzimidazole compounds (16 – 42) using the polyphosphoric acid method. These compounds were screened for their antibacterial activity and their antifungal activity. Compound 25 showed maximum potency against both Gram-positive and Gram-negative bacterial strains with minimum inhibitory concentration (MIC) values in the range of 7.81 – 31.25 μg/mL. In particular, it showed the maximum MIC values of 7.81 μg/mL against Gram-negative bacteria, which was four-fold more active than the standard drug ampicillin (MIC = 32.25 μg/mL). Compound 19 was found to be the most active against S. aureus with a MIC value of 3.90 μg/mL, whereas the remaining compounds showed only low-to-moderate activity. Furthermore, all compounds exhibited low activity against all fungal strains in comparison to the standard drug fluconazole. I addition, pharmacophore hypotheses were generated to analyze structure–activity relationships between the molecular structures and antimicrobial activities on E. coli. This pharmacophore model can be useful in order to design new antimicrobial drugs. It can be suggested that the substitution of a phenyl ring at the 5/6 and 5′/6′ positions in symmetric bisbenzimidazole derivatives produces compounds with promising antimicrobial activity.
CuO nano-particles supported on silica, a new catalyst for facile synthesis of benzimidazoles, benzothiazoles and benzoxazoles
Inamdar, Suleman M.,More, Vinod K.,Mandal, Sisir K.
, p. 579 - 583 (2013/02/23)
A facile synthetic route for benzimidazoles, benzothiazoles and benzoxazoles comprising the reaction of corresponding o-phenylenediamine, o-aminothiophenol and o-aminophenol with various aldehydes using silica supported nano-copper (II) oxide as a catalyst has been described. The catalyst exhibited clean reaction profile with excellent yields in a short reaction time. The catalyst can be recycled effectively after use.
Synthesis and anti-HIV activity of [ddN]-[ddN] dimers and benzimidazole nucleoside dimers
Li, Guo-Rui,Liu, Jun,Pan, Qin,Song, Zhi-Bin,Luo, Feng-Ling,Wang, Shao-Ru,Zhang, Xiao-Lian,Zhou, Xiang
scheme or table, p. 2200 - 2208 (2010/07/17)
In an attempt to combine the HIV-inhibitory capacity of different 2′,3′-dideoxynucleoside (ddN) analogs, we have designed and synthesized several dimers of [AZT]-[AZT] and [AZT]-[d4T]. In addition, we also synthesized the dimers of 1-(1H-benzimidazol-1-yl