97420-40-1Relevant academic research and scientific papers
Synthesis and Antibacterial Activity of Some Derivatives of 2-Methylbenzimidazole Containing 1,3,4-Oxadiazole or 1,2,4-Triazole Heterocycle
Nguyen Tien, Cong,Tran Thi Cam, Duc,Bui Manh, Ha,Nguyen Dang, Dat
, (2016/03/05)
5-[(2-Methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-oxadiazole-2-thiol or 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-4-(4-methylphenyl)-1,2,4-triazol-3-thiol which were prepared starting from 2-methylbenzimidazole in the reaction with appropriate N-aryl-2-chlo
Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity
Khan, Imran,Tantray, Mushtaq A.,Hamid, Hinna,Alam, Mohammad Sarwar,Kalam, Abul,Dhulap, Abhijeet
supporting information, p. 4020 - 4024 (2016/08/01)
A series of benzimidazole based thiadiazole and carbohydrazide conjugates have been synthesized and evaluated for inhibition of glycogen synthase kinase-3β and anti-depressant effect. Compounds 4f, 4j, 5b, 5g and 5i were found to be the most potent inhibitors of GSK-3β in vitro amongst the twenty-five benzimidazole based thiadiazole and carbohydrazide conjugates synthesized. Compound 5i was also found to exhibit significant antidepressant activity in vivo at 50?mg/kg, when compared to fluoxetine, a known antidepressant drug. The molecular docking studies revealed multiple hydrogen bond interactions by the synthesized compounds with various amino acid residues, viz, ASP-133, LYS-183, PRO-136, VAL-135, TYR-134, or LYS-60 at the GSK-3β receptor site.
Structure-activity studies of divin: An inhibitor of bacterial cell division
Zhou, Maoquan,Eun, Ye-Jin,Guzei, Ilia A.,Weibel, Douglas B.
supporting information, p. 880 - 885 (2013/10/01)
We describe the synthesis and structure-activity relationship (SAR) studies of divin, a small molecule that blocks bacterial division by perturbing the assembly of proteins at the site of cell septation. The bacteriostatic mechanism of action of divin is distinct from other reported inhibitors of bacterial cell division and provides an opportunity for assessing the therapeutic value of a new class of antimicrobial agents. We demonstrate a convenient synthetic route to divin and its analogues, and describe compounds with a 10-fold increase in solubility and a 4-fold improvement in potency. Divin analogues produce a phenotype that is identical to divin, suggesting that their biological activity comes from a similar mechanism of action. Our studies indicate that the 2-hydroxynaphthalenyl hydrazide portion of divin is essential for its activity and that alterations and substitution to the benzimidazole ring can increase its potency. The SAR study provides a critical opportunity to isolate drug resistant mutants and synthesize photoaffinity probes to determine the cellular target and biomolecular mechanism of divin.
Synthesis and biological activity of some triazole-bearing benzimidazole derivatives
Ansari,Lal,Khitoliya
scheme or table, p. 341 - 352 (2012/01/05)
A number of N'-(arylmethylidene)-2-(2-methyl-1H-benzimidazol- -1-yl)acetohydrazide and 4-aryl-5-[(2-methyl-1H-benzimidazol-1-yl)methyl]- -4H-1,2,4-triazole-3-thiol derivatives were synthesized by incorporating various aromatic and heterocyclic substituents on 2-methyl-1H-benzimidazole. The structures of all the synthesized compounds were elucidated based on their elemental analyses and spectral data. The in vitro activities of these compounds against bacteria and fungi were evaluated by the disc diffusion and the minimum inhibitory concentration (MIC) methods. Some of the synthesized derivatives were found to be as active as kanamycin (standard drug).
Synthesis, physicochemical properties and antimicrobial activity of some new benzimidazole derivatives
Ansari,Lal
experimental part, p. 4028 - 4033 (2009/12/04)
Some derivatives of benzimidazole were synthesized by nucleophilic substitution of 2-substituted-1H-benzimidazole. The resulting ethyl (2-substituted-1H-benzimidazol-1-yl) acetate on treatment with hydrazine hydrate yielded 2-(2-substituted-1H-benzimidazol-1-yl) acetohydrazide, which on further reaction with one equivalent of different aliphatic or aromatic carboxylic acids in the presence of phosphoryl chloride afforded the corresponding target compounds, 2-substituted-1-[{(5-substituted alkyl/aryl)-1,3,4-oxadiazol-2-yl} methyl]-1H-benzimidazole. The structures of the synthesized compounds were evaluated by spectral and elemental methods of analyses. All the synthesized compounds were screened for their antimicrobial activities. All of the derivatives showed good activity towards Gram-positive bacteria and negligible activity towards Gram-negative bacteria. Some of the synthesized compounds showed moderate activity against tested fungi.
Synthesis find biological activity of new benzimidazoles
Shetgiri,Kokitkar
, p. 163 - 166 (2007/10/03)
A series of 1-[(4- (4′-substituted)phenyl-3-alkyl/aralkyl-thio4H-1,2,4-triazol-5-yl) methyl]-2-methyl-1H-benzimidazoles (6aa-6ag, 6ba-6bg, 6ca-6cg) has been synthesized. The compounds are characterized and screened for their antimicrobial activity.
Research In The Imidazole Series. 93. Synthesis Of Derivatives Of Benzimidazolyl-1-Acetic Acid
Kochergin, P. M.,Palei, R. M.,Chernyak, S. A.
, p. 560 - 562 (2007/10/02)
A simple method has been developed for obtaining esters of benzimidazolyl-1-acetic acid and its 2-alkyl (or aralkyl) derivatives, by reaction of benzimidazoles with esters of chloroacetic or bromoacetic acid in DMF in the presence of anhydrous potassium c
