A series of novel benzimidazole derivatives were synthesized and characterized by (1)H NMR, (13)C NMR, MS, IR and HRMS spectra. All the new compounds were screened for their antimicrobial activities in vitro by two-fold serial dilution technique. Bioactive assay manifested that the bis-benzimidazole derivative 11d and its hydrochloride 13b exhibited remarkable antimicrobial activities, which were comparable or even better than the reference drugs Norfloxacin, Chloromycin and Fluconazole. The interaction evaluation of compound 11d with bovine serum albumin (BSA) by Fluorescence and UV-vis absorption spectroscopic method showed that BSA could generate fluorescent quenching under approximately human physiological conditions by the prepared benzimidazole compound 11d as result of the formation of ground-state compound 11d-BSA complex. The thermodynamic parameters indicated that the hydrogen bonds and van der Waals forces played major roles in the strong association of benzimidazole 11d and BSA.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2012.07.015 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The challenge of treating hepatitis C virus infection in children with comorbidities.
Eur J Pediatr
March 2025
Pediatric Hepatology Unit, Department of Pediatrics, Cairo University, Cairo, Egypt.
Unlabelled: Direct-acting antivirals (DAAs) have revolutionized hepatitis C virus (HCV) treatment and enabled the treatment of those who could not be treated using interferon. The aim of this work was to assess the efficacy and safety of oral DAAs in HCV-infected children with associated comorbidities. This analytical retrospective study included children with HCV mono-infection versus those with associated comorbidities.
View Article and Find Full Text PDFPredicting the anticancer activity of indole derivatives: A novel GP-tree-based QSAR model optimized by ALO with insights from molecular docking and decision-making methods.
Comput Biol Med
March 2025
Biomaterials and Transport Phenomena Laboratory, Faculty of Technology, University Yahia Fares of Medea, 26000, Medea, Algeria; Laboratory of Quality Control, Physico-Chemical Department, SAIDAL of Medea, Medea, Algeria.
Indole derivatives have demonstrated significant potential as anticancer agents; however, the complexity of their structure-activity relationships and the high dimensionality of molecular descriptors present challenges in the drug discovery process. This study addresses these challenges by introducing a modified GP-Tree feature selection algorithm specifically designed for regression tasks and high-dimensional feature spaces. The algorithm effectively identifies relevant descriptors for predicting LogIC values, the target variable.
View Article and Find Full Text PDFSustainable Synthesis of Polyfluoro-Pyrimido [1,2-] Benzimidazole Derivatives Using a Tandem Strategy─Ultrasound and an Integrated Continuous Flow System.
J Org Chem
March 2025
Department of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung 80708, Taiwan ROC.
We have developed a novel ultrasound technique that generates significant amounts of CF-substituted benzo[4,5] imidazo [1,2-]pyrimidine analogues from easily accessible starting materials in an ecologically friendly and efficient approach. This method is notably helpful for producing physiologically relevant compounds containing the imidazopyrimidine unit, which serves as a versatile building block for the synthesis of -fused heterocycles and is devoid of metals, solvents, additives, and catalysts. Additionally, utilizing ultrasound in an open-air environment, a range of polyfluoro-ynones were successfully reacted with 2-aminobenzimidazole, generating a diverse array of polyfluoroimidazo[1,2-]pyrimidine derivatives.
View Article and Find Full Text PDFTargeted degradation of CDK4/6 by LA-CB1 inhibits EMT and suppresses tumor growth in orthotopic breast cancer.
Sci Rep
March 2025
Cancer Center and Department of Pharmacology and Toxicology, Medical College of Wisconsin, Milwaukee, WI, 53226, USA.
Cyclin-dependent kinases 4 and 6 (CDK4/6) are central regulators of cell cycle progression and frequently dysregulated in cancers, including breast cancer. While selective CDK4/6 inhibitors like Palbociclib, Ribociclib, and Abemaciclib have shown clinical benefit in hormone receptor-positive (HR+) breast cancer, their efficacy is often limited by resistance mechanisms and dose-limiting toxicities. In this study, we developed LA-CB1, a novel Abemaciclib derivative that induces CDK4/6 degradation through the ubiquitin-proteasome pathway, aiming to achieve sustained inhibition of the CDK4/6-Rb axis.
View Article and Find Full Text PDFGold Nanoparticles Functionalized With 5-Amino-2-Mercaptobenzimidazole: A Promising Antimicrobial Strategy Against Carbapenem-Resistant Gram-Negative Bacteria.
Int J Nanomedicine
March 2025
School of Laboratory Medicine and Life Science, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.
Introduction: Carbapenem-resistant gram-negative bacteria (CR-GNB) pose a significant threat to public health and require immediate attention. The development of novel antibacterial agents against CR-GNB has become an urgent priority, and nanomaterials offer promising solutions due to their unique properties. This study introduces 5-amino-2-mercaptobenzimidazole (5-A-2MBI) functionalized gold nanoparticles (5-A-2MBI_Au NPs) and evaluates their antibacterial activity against CR-GNB.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!