Synthesis, molecular docking, antibacterial, and anti‐inflammatory activities of benzimidazole‐containing tricyclic systems. Issue 6 (27th January 2021)

• Record Type: Journal Article
• Authors: Kamat, Vinuta; Yallur, Basappa C.; Poojary, Boja; Patil, Veerabhadragouda B.; Nayak, Suresh P.; Krishna, Panchangam Murali; Joshi, Shrinivas D.
• Is Part Of: Journal of the Chinese Chemical Society. Volume 68:Issue 6(2021)
• Page Start: 1055
• Page End: 1066
• Publication Date: 2021-01-27
• Subjects: benzimidazole -- molecular docking -- pharmacokinetics -- tricyclic; Chemistry -- Periodicals; Electronic journals; 540.5
• DOI: 10.1002/jccs.202000454
• Languages: English
• ISSNs: 0009-4536

Abstract

Abstract: In the present study, we reported the synthesis of benzimidazole‐containing tricyclic systems and evaluated their antimicrobial efficacy against some Gram‐positive, Gram‐negative strains, and their anti‐inflammatory activity as well as a hemolytic assay in terms of percentage. The antimicrobial study of the synthesized compounds revealed that most of them showed significant activity, and compound 5b displayed excellent antimicrobial efficacy among all. Results showed that the hydroxyl group at the fourth position on the aromatic ring has a substantial role in the biological activity. Synthesized compounds showed promising minimum inhibitory concentration ( μ g/mL) values in the range of 1.2–12.8 μ g/mL against the tested strains. The in vitro anti‐inflammatory activity of these compounds was evaluated by denaturation of bovine serum albumin method and showed the inhibition in the range of IC50 value 31.16–94.63 μ g/mL. Among all the tested compounds, compound 5b has a significant IC50 value. The percentage of hemolysis of the target compounds ranged from 1.14 to 52.8 at a concentration of 100 μ g/mL. Molecular docking study revealed the good binding interactions against Escherichia coli, and it is best suited with in vitro studies. Pharmacokinetic studies showed the safe profiles for the title compounds. Abstract : In the present study, we successfully synthesized some tricyclic benzimidazole containing scaffolds. Further, they were screened for their antimicrobial and in vitro anti‐inflammatory study, results shown good efficiency. The percentage hemolysis of the target compounds reveals that compounds were nontoxic.