Design, Microwave‐Assisted Synthesis and in Vitro Antibacterial and Antifungal Activity of 2,5‐Disubstituted Benzimidazole

Abstract

Seventeen novel 2,5‐disubstituted benzimidazole derivatives were designed, synthesized and evaluated for their antibacterial activities. The tested compounds B1–B4 and C2–C6 exhibited not only good antifungal activity but also favorable broad‐spectrum antibacterial activity. Also, the lowest MIC of antibacterial and antifungal activity was 2 μg/mL and 4 μg/mL, respectively. It suggested that the structure of compound including the different substituent and its sites directly affected the efficacy of the synthesized compounds.

Screening and Identification of a Novel Anti-tuberculosis Compound That Targets Deoxyuridine 5′-Triphosphate Nucleotidohydrolase

“…F0414 is a benzimidazole compound with no biological activities reported. There has been a lot of benzimidazole compounds used in clinic, which exhibited various properties, such as anti-tumor, anti-viral, anti-bacterial, anti-fungal, and anti-metabolic syndrome ( He et al, 2019 ; Shi et al, 2019 ; Singh et al, 2019 ; Tharmalingam et al, 2019 ). For example, pracinostat, a novel benzimidazole-based histone deacetylase inhibitor, has been identified as a potential agent for treating breast cancer ( Chen et al, 2020 ).…”

A Magnetic Fe3O4/Modified Bentonite Composite as Recyclable Heterogeneous Catalyst for Synthesizing 2‐Substituted Benzimidazoles

“…2‐(pyridin‐3‐yl)‐1 H ‐benzo[d]imidazole : [61] m=0.327 g. 1 H NMR (400 MHz, DMSO‐ d 6 ) δ (ppm): 13.12 (s, 1H), 9.38 (s, 1H), 8.70 (s, 1H), 8.52 (s, 1H), 7.63 (s, 3H), 7.26 (s, 2H). HRMS (EI): Calcd for C 13 H 9 N 3 [M+H] + 196.0869, found 196.0877.…”

Recent achievements in the synthesis of benzimidazole derivatives

“…A wide range of products was obtained in moderate to excellent yields under microwave irradiation. 133 Some synthesized compounds showed strong antibacterial and antifungal activity ( Scheme 64 ). Bioassay study revealed that several synthesized compounds exhibited good antifungal activity and broad-spectrum antibacterial activity.…”