Synthesis, antimicrobial evaluation and docking studies of fluorinated imine linked 1,2,3-triazoles

Kumar, Aman; Lal, Kashmiri; Poonia, Nisha; Kumar, Ashwani; Kumar, Anil

doi:10.1007/s11164-022-04737-2

Cited by 19 publications

(2 citation statements)

References 48 publications

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“…Similarly, the halogenated azoles (Fig. 10V-W) targeted sterol 14-α demethylase to exhibit anticandidal activity and DNA gyrase to inhibit E. coli (Kumar et al, 2022). Also, 10Z is effectively intercalated into DNA to block replication in E. coli and could be transported by human serum albumin in the blood plasma via electrostatic interactions to enhance the drug distribution (Lv et al, 2014).…”

Section: E Azolesmentioning

confidence: 99%

Halogenated Antimicrobial Agents to Combat Drug-Resistant Pathogens

Faleye,

Boya,

Lee

et al. 2023

Pharmacol Rev

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Antimicrobial resistance presents us with a potential global crisis as it undermines the abilities of conventional antibiotics to combat pathogenic microbes. The history of antimicrobial agents is replete with examples of scaffolds containing halogens. In this review, we discuss the impacts of halogen atoms in various antibiotic types and antimicrobial scaffolds and their modes of action, structure-activity relationships, and the contributions of halogen atoms in antimicrobial activity and drug resistance. Other halogenated molecules, including carbohydrates, peptides, lipids, and polymeric complexes, are also reviewed, and the effects of halogenated scaffolds on pharmacokinetics, pharmacodynamics, and factors affecting antimicrobial and antivirulence activities are presented. Furthermore, the potential of halogenation to circumvent antimicrobial resistance and rejuvenate impotent antibiotics is addressed. This review provides an overview of the significance of halogenation, the abilities of halogens to interact in biomolecular settings and enhance pharmacological properties, and their potential therapeutic usages in preventing a post-antibiotic era. Significance StatementAntimicrobial resistance and the increasing impotence of antibiotics are critical threats to global health. The roles and importance of halogen atoms in antimicrobial drug scaffolds have been established, but comparatively little is known of their pharmacological impacts on drug resistance and antivirulence activities. This review is the first to extensively evaluate the roles of halogen atoms in various antibiotic classes and pharmacological scaffolds and to provide an overview of their abilities to overcome antimicrobial resistance.

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Section: E Azolesmentioning

confidence: 99%

Halogenated Antimicrobial Agents to Combat Drug-Resistant Pathogens

Faleye,

Boya,

Lee

et al. 2023

Pharmacol Rev

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“…Hence, it may prove to be a better candidate for pharmacological applications. [96][97][98][99][100] Recently, copper has been used in the enantioselective synthesis of imines. [101] A fluorescent sensor based on a cross-reactive aliphatic imine receptor has also been investigated recently.…”

Section: Our Perspectives and Future Prospectsmentioning

confidence: 99%

A Comprehensive Review on Cu‐Catalysed Aerobic Oxidation of Amines to Imines

2023

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Imines are frequently used as valuable intermediates in organic transformation and pharmaceutical synthesis. Conventional imine synthesis includes Lewis acid catalysts, dehydrating agents, and unstable aldehydes. Developing eco‐friendly molecular assembly techniques has become increasingly important in recent years. In particular, there is a significant need for methods that recycle resources and have high atomic efficiency with minimal environmental impact. Oxidative synthesis of imines from amines has been investigated in presence of molecular oxygen (or air) which is readily accessible on Earth. The closely linked catalysts have been classified into metals, bio‐inspired, and MOF catalysts. Highly active, affordable, and adaptable copper based catalysts are given special attention here, some critical elements that influence reaction processes and catalytic activity are also displayed in the present study. The modern methods along with mechanistic routes for converting primary amines to imines using copper catalytic systems and ambient oxygen have been discussed in detail.

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