Anion-driven C F bond cleavage of trifluoromethyl N-aryl hydrazones toward the assembly of N-heterocycles DOI
Qijie Zou, Qingyu Meng, Jingyuan Wang

et al.

Tetrahedron Letters, Journal Year: 2024, Volume and Issue: 151, P. 155328 - 155328

Published: Oct. 11, 2024

Language: Английский

Photo-induced decarboxylative radical cascade cyclization of unactivated alkenes: access to CF- and CF2-substituted ring-fused imidazoles DOI Creative Commons
Hui-Nan Wang, Shaohui Lin, Hui Hong

et al.

RSC Advances, Journal Year: 2025, Volume and Issue: 15(16), P. 12739 - 12745

Published: Jan. 1, 2025

A mild and effective visible-light-induced decarboxylative radical cascade reaction of olefin-containing imidazoles α-fluorinated carboxylic acids, has been developed to afford monofluoromethylated or aryldifluoromethylated polycyclic imidazoles.

Language: Английский

Citations

0
Design and synthesis of new benzimidazole-hybrids as anti-microbial agents: exploring the mechanistic insights as DNA gyrase inhibitors via in silico and in vitro based studies DOI
Anand Maurya, Upendra Kumar Patel,

Punit Tiwari

et al.

Journal of Biomolecular Structure and Dynamics, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 20

Published: May 13, 2025

Two series of antibacterial agents, 1,2,3-triazole and aminopyrimidine benzimidazole hybrids, were designed, synthesized, characterized by IR, NMR, Mass spectroscopy, X-ray crystallography studies. The biological studies revealed that compounds 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 8d, 8e, 9d, 9e, 9f, 9h, 9j, 9k exhibited significant activity in vitro compared to the standard drug ciprofloxacin, against Gram-positive Gram-negative bacterial strains. study hemotoxicity displayed a negligible toxicity profile for all compounds. Furthermore, mechanistic insights predicted via molecular docking on DNA gyrase (Glide Scores) 5c 5f possess better affinity within active domain gyrase, which was further corroborated using dynamics followed direct gyrase-based inhibition assays. Compound most potent, while showed an equipotent drug.

Language: Английский

Citations

0
Synthesis and evaluation of di‐heterocyclic benzazole compounds as potential antibacterial and anti‐biofilm agents against Staphylococcus aureus DOI Creative Commons

Mine Buga Aktekin,

Zehra Öksüz, Burçin Türkmenoğlu

et al.

Chemical Biology & Drug Design, Journal Year: 2024, Volume and Issue: 104(2)

Published: July 31, 2024

Abstract Cumulative escalation in antibiotic‐resistant pathogens necessitates the quest for novel antimicrobial agents, as current options continue to diminish bacterial resistance. Herein, we report synthesis of di‐heterocyclic benzazole structures ( 12–19 ) and their vitro evaluation some biological activities. Compounds 16 17 demonstrated potent antibacterial activity (MIC = 7.81 μg/mL) against Staphylococcus aureus , along with significant anti‐biofilm activity. Noteworthy is capability Compound inhibit biofilm formation by at least 50% sub‐MIC (3.90 concentration. Furthermore, both compounds exhibited potential preformed MIC concentration (7.81 μg/mL). Additionally, were examined cytotoxic effects HFF‐1 cells, using MTT method, screened binding interactions within active site S. DNA gyrase silico molecular docking technique, employing AutoDock 4.2.6 Schrödinger Glidse programs. Overall, our findings highlight promising scaffolds warranting further optimization development effective agents.

Language: Английский

Citations

1
Investigation of Benzimidazole Derivatives in Molecular Targets for Breast Cancer Treatment: A Comprehensive review DOI

P Katiyar,

Kalpana Kalpana,

Aditi Srivastava

et al.

Critical Reviews™ in Oncogenesis, Journal Year: 2024, Volume and Issue: 30(1), P. 43 - 58

Published: Nov. 6, 2024

This article provides a basic summary of computational research on benzimidazole and its molecular targets in breast cancer (BC) drug discovery. The development process is streamlined, expenses are decreased, the possibility finding successful therapies for this difficult illness increased with use tools. utilization derivatives medication discovery discussed, along results derivative-related clinical trials conducted against blood during previous five years. Additionally, it includes analysis changes structure how they affect pharmacology. structure-based method other tools used also covered, as well importance structural information such stereochemistry, physiological action, spectroscopic methods like NMR X-ray crystallography understanding interactions between bioactive compounds receptors. highlights potential benzimidazoles heterocyclic molecules various biological activities, including antimicrobial anti-cancer properties.

Language: Английский

Citations

1
Anion-Driven C-F Bond Cleavage of Trifluoromethyl N -Aryl Hydrazones Toward the Assembly of N-Heterocycles DOI
Fangyi Li, Qijie Zou, Qingyu Meng

et al.

Published: Jan. 1, 2024

An efficient and convenient synthesis of 1H-benzo[d]imidazoles has been developed by employing a base-promoted transformation readily available α-CF3 ketone-derived hydrazones with o-phenylenediamines. The strategy involves anion-driven triple-cleavage C-F bond the CF3 group attached to N-arylhydrazones, which acts as C1 synthon at 2-position 1H-benzo[d]imidazoles. Furthermore, present synthetic method can be generalized access benzo[d]oxazoles benzo[d]thiazoles.

Language: Английский

Citations

0
Anion-driven C F bond cleavage of trifluoromethyl N-aryl hydrazones toward the assembly of N-heterocycles DOI
Qijie Zou, Qingyu Meng, Jingyuan Wang

et al.

Tetrahedron Letters, Journal Year: 2024, Volume and Issue: 151, P. 155328 - 155328

Published: Oct. 11, 2024

Language: Английский

Citations

0