Synthesis and Antibacterial Activity of Novel 2-Oxo-pyrrolidinyl Oxazolidinones

Bhattarai, Deepak; Lee, Sun Hee; Kim, Hyeong Kyu; Kang, Seonmi; Pae, Ae Nim; Kim, Eunice EunKyeong; Oh, Tae-Ho; Cho, Sang Nae; Keum, Gyochang

doi:10.5012/bkcs.2012.33.4.1310

Cited by 2 publications

(2 citation statements)

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“…Mutations of the 23S rRNA of the 50S ribosomal diminish oxazolidinone affinity and antibiotic resistance. Several synthesized halogenated oxazolidinone derivatives, such as derivatives with a halogenated pyrrolidone moiety at αor β-position, have exhibited antimicrobial activity against drug-resistant MRSA, vancomycinresistant Staphylococcus aureus, and several other Gram-negative bacteria (Bhattarai et al, 2012). No significant changes were observed in the MICs of these derivatives against drugsensitive and drug-resistant strains except S. aureus strains which had a two-fold increase in MICs against resistant strains.…”

Section: Lincosamides and Oxazolidinones)mentioning

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: Lincosamides and Oxazolidinones)mentioning

confidence: 99%

Halogenated Antimicrobial Agents to Combat Drug-Resistant Pathogens

Faleye,

Boya,

Lee

et al. 2023

Pharmacol Rev

View full text Add to dashboard Cite

show abstract

“…To improve the potency and broaden the spectrum of oxazolidinone antibacterials, [25][26][27] we reported previously that modification of the morpholine C-ring of linezolid with an azabicylo [3.3.0] octanyl group as a conformationally constrained isostere enhanced in vitro antibacterial activity, which was comparable or superior to linezolid against Gram-positive bacteria and M. tuberculosis. Herein, we described the synthesis of novel oxazolidinones bearing an octahydrocyclopenta[c]-pyrrol-2-yl ring with a stereoselective oxygen or nitrogen substituent at the 5-position, as shown in Fig.…”

Section: Synthesis and In Vitro Evaluation Of The Antitubercular And mentioning

confidence: 99%