Synthesis and Pharmacological Investigations of Novel Pyrazolyl and Hydrazonoyl Cyanide Benzimidazole Entities

Abstract

in Wiley Online Library (wileyonlinelibrary.com).Various novel benzimidazole entities linked to pyrazolyl and hydrazonoyl cyanide substrates carrying aryl and heteroaryl groups (8a-e to 10a-e) were synthesized using new route syntheses and were focused on their pharmacological evaluation as one of the most important factors for the determination of the activity of these synthesized compounds. The obtained benzimidazoles' series were fully characterized and exhibited remarkable pharmacological activity upon in vitro screening for their antibacterial activity against strains of selected pathogenic Gram-positive bacteria (Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli) comparing with Ampicillin and Kanamycin as standard antibacterial agents and against human liver cancer cell lines (HepG2) as antitumor agents as well.

Synthesis and comparative solvatochromic studies of novel Mono azo ureido/thioureido benzimidazole dyes

“…Chemistry Synthesis of hydrazonoyl bromide derivatives (3a-c) is preceded by routine coupling reaction of freshly diazotized aromatic amines (2a-c) with BMB (1) (Khalifa et al, 2019) as a coupler component (Scheme 1). Although the simplicity of this idea, the compounds (3a-c) are found to be novel as per Scifinder structure search.…”

“…Benzimidazoles are the corner stones as intermediates in many organic reactions (Bai et al , 2001; Hasegawa et al , 1999), important synthons for modeling many biological systems (Erhardt, 1987; Gravatt et al ,1994; Jayabharathi et al , 2013; Khalifa, 2020; Khalifa et al , 2019; Roth et al , 1997) and in supramolecular host-guest systems for Nanomedicine (Praveen and Babu, 2019; Wu et al , 2015). Their characteristic optical linear (Praveen et al , 2015) and second-order non-linear properties (Batista et al , 2007) have been studied and could to be boosted by planting hydroxyl and/or alkoxy substituents (Krawczyk, 2020).…”

Synthesis and Evaluation of New 2‐Mercaptomethyl Benzimidazole Scaffolds as Potential Antibacterial, Antioxidant and Cytotoxic Agents

“…Relying on the highly importance and varied bioactivities exhibited by benzimidazoles, efforts have been made to generate many derivatives and screened them for potential biological activities. In continuation of our earlier studies for design and synthesize potent compounds with antimicrobial and antitumor efficiency including benzimidazole derivatives and extensive literature survey, it is worthwhile to design and synthesize novel derivatives based on 2‐mercaptobenzimidazole moiety by convenient methods. The new compounds are fully characterized by various spectral analyses followed by their screening as potential anti bacterial (i. e. Staphylococcus aureus; S. aureus and Escherichia coli; E. coli) , antioxidant and anti‐human hepatocellular carcinoma (HEP−G2) activities comparing with standard commercial drugs.…”

Discovery of novel natural products as dual MNK/PIM inhibitors for acute myeloid leukemia treatment: Pharmacophore modeling, molecular docking, and molecular dynamics studies

“…Natural products (NPs) have shown great activity against various diseases; their use is explained by many advantages, including antiapoptotic, anti-inflammatory, cardioprotective, cosmological use, and others (Scotti et al, 2017;Koch et al, 2019;Antiviral, 2020;Tao et al, 2020;Wu et al, 2021). In recent years, NPs have been important sources of anticancer agents; not only for their structural variety and high activity but also for their greater selectivity and low side effects when compared to conventional cancer therapy (synthetic ones) (Khalid et al, 2016;Ruiz-Torres et al, 2018;Khalifa et al, 2019;Alam et al, 2021). Some NPs were also found to be effective in the treatment of MDR resistance (Banik et al, 2021).…”