Author(s):
Tushar R. Chandan, Ayaz Aadam Shah, Hitesh C. Shelar, Kavita M. Choudhari
Email(s):
tusharchandan510@gmail.com
DOI:
10.52711/0974-4150.2026.00057 
Address:
Tushar R. Chandan1*, Ayaz Aadam Shah3, Hitesh C. Shelar2, Kavita M. Choudhari1
1Department of Pharmacology, K. K. Wagh Education Society, K. K. Wagh College of Pharmacy, Nashik – 422003, Maharashtra, India.
2Department of Pharmaceutical Chemistry, K. K. Wagh Education Society, K. K. Wagh College of Pharmacy, Nashik - 422003, Maharashtra, India.
3Department of Pharmaceutical Chemistry, SSS’s Divine College of Pharmacy, Nampur Road, Satana, Maharashtra, India - 423301.
*Corresponding Author
Published In:
Volume - 19,
Issue - 4,
Year - 2026
ABSTRACT:
Due to the increase in global antimicrobial resistance (AMR), there has been a need to create new classes of antibacterials to treat resistant Gram-positive organisms. The first clinically relevant oxazolidinone, linezolid, was a true game changer due to its synthetic nature and novel mechanism of action by targeting initiation of bacterial ribosome formation. Linezolid is believed to have an ant staphylococcal effect by binding to domain V of 23S rRNA within the 50S ribosomal subunit thus preventing formation of the 70S initiation complex. The drug has significant activity against multidrug resistant Gram-positive pathogens, such as methicillin resistant staphylococcus aureus and vancomycin resistant enterococci. Linezolid has very good oral bioavailability, predictable pharmacokinetic parameters, and good tissue penetration; however, prolonged use is associated with the development of myelosuppression, mitochondrial toxicity, and emerging resistance mechanisms due to 23S rRNA mutations and cfr gene methylation. Linezolid is still a major drug of choice for many infections caused by resistant Gram-positive bacteria, but the changes in resistance patterns over time warrant further evaluation of the safety and efficacy of linezolid.
Cite this article:
Tushar R. Chandan, Ayaz Aadam Shah, Hitesh C. Shelar, Kavita M. Choudhari. Linezolid: Chemical Evolution, Mechanistic Pharmacology, Clinical Utility, Resistance Dynamics, and Future Oxazolidinone Strategies. Asian Journal of Research in Chemistry.2026; 19(4):377-0. doi: 10.52711/0974-4150.2026.00057
Cite(Electronic):
Tushar R. Chandan, Ayaz Aadam Shah, Hitesh C. Shelar, Kavita M. Choudhari. Linezolid: Chemical Evolution, Mechanistic Pharmacology, Clinical Utility, Resistance Dynamics, and Future Oxazolidinone Strategies. Asian Journal of Research in Chemistry.2026; 19(4):377-0. doi: 10.52711/0974-4150.2026.00057 Available on: https://www.ajrconline.org/AbstractView.aspx?PID=2026-19-4-14
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