• 1. Advances in predicting organic contaminant abatement during ozonation of municipal wastewater effluent: reaction kinetics, transformation products, and changes of biological effects
  Yunho Lee,Urs von Gunten Environ. Sci.: Water Res. Technol. 2016 2 421

• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Quinolines and derivatives Quinoline carboxylic acids

Desmethyl levofloxacin (CAS No. 117707-40-1): A Comprehensive Overview

Desmethyl levofloxacin, chemically identified by the CAS number 117707-40-1, is a significant metabolite and intermediate in the pharmacokinetic profile of the widely used fluoroquinolone antibiotic, levofloxacin. This compound has garnered considerable attention in the field of pharmaceutical chemistry and medicinal biology due to its unique structural properties and potential therapeutic applications. Understanding its chemical structure, biological significance, and emerging research findings provides valuable insights into its role in drug metabolism and development.

The molecular formula of Desmethyl levofloxacin is C₁₈H₁₈F₃N₃O₄, reflecting its structural similarity to levofloxacin with the addition of a methyl group at the 6-position of the quinolone ring. This modification imparts distinct pharmacokinetic and pharmacodynamic characteristics, making it a subject of intense study in drug metabolism and pharmacogenetics. The compound's stability, solubility, and interaction with biological targets are critical factors that influence its potential as a therapeutic agent or a biomarker for drug efficacy and safety.

In recent years, advancements in analytical techniques such as liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR) spectroscopy have enabled more precise characterization of Desmethyl levofloxacin. These methods have been instrumental in elucidating its metabolic pathways and identifying key enzymes involved in its formation and degradation. For instance, cytochrome P450 enzymes, particularly CYP1A2 and CYP3A4, have been implicated in the demethylation of levofloxacin to produce Desmethyl levofloxacin, highlighting the importance of these enzymes in individualizing patient therapy based on genetic variability.

The biological activity of Desmethyl levofloxacin has been a focus of numerous studies aiming to understand its contribution to the overall therapeutic effect of levofloxacin. While it exhibits lower antibacterial activity compared to its parent compound, research suggests that it may still possess significant pharmacological properties. Studies have indicated that Desmethyl levofloxacin could interfere with bacterial DNA gyrase and topoisomerase IV, similar to levofloxacin, albeit with reduced efficacy. This finding underscores the complexity of fluoroquinolone metabolism and the need for comprehensive understanding to optimize therapeutic outcomes.

The pharmacokinetic behavior of Desmethyl levofloxacin is another area of active investigation. Its half-life, distribution volume, and clearance rates are influenced by various factors including age, renal function, and genetic polymorphisms. For instance, patients with impaired renal function may exhibit higher levels of this metabolite due to reduced clearance rates, potentially leading to increased adverse effects. Such findings emphasize the importance of monitoring metabolite levels in clinical settings to ensure safe and effective dosing regimens.

In the context of drug development, Desmethyl levofloxacin serves as a valuable biomarker for assessing drug-drug interactions and individualizing therapy. Its formation can be affected by concomitant medications that inhibit or induce cytochrome P450 enzymes, leading to significant variations in metabolite levels. This has implications for patients receiving multiple medications simultaneously, as it may necessitate dose adjustments or alternative therapeutic strategies to minimize potential adverse effects.

The role of Desmethyl levofloxacin in clinical research has also expanded beyond its role as a metabolite. Emerging evidence suggests that it may have distinct therapeutic applications in certain conditions. For example, studies have explored its potential use in combination therapies targeting resistant bacterial strains. The unique pharmacological profile of this metabolite could enhance the efficacy of existing antibiotics by acting on different bacterial targets or mechanisms.

The synthesis and characterization of synthetic analogs of Desmethyl levofloxacin have opened new avenues for drug discovery. By modifying specific structural features while retaining key pharmacophores, researchers aim to develop novel compounds with improved efficacy, reduced side effects, or enhanced target specificity. These efforts are supported by computational modeling techniques that predict binding interactions between the metabolite analogs and biological targets such as bacterial enzymes.

The regulatory landscape for compounds like Desmethyl levofloxacin is another critical consideration in pharmaceutical development. Regulatory agencies require comprehensive data on their safety profiles before approving new drugs or approving new indications for existing ones. This includes toxicological studies evaluating potential long-term effects as well as clinical trials demonstrating efficacy in specific patient populations.

In conclusion,< strong.Desmethyl levofloxacin (CAS No. 117707-40-1) strong>.is more than just a metabolic byproduct; it is a multifaceted compound with significant implications for drug metabolism,bioavailability,and therapeutic applications.Despite extensive research,the full potential and challenges associated with this metabolite remain areas for further exploration.Future studies should continue to unravel its complex interactions within biological systems while exploring novel ways to leverage its properties for improved patient care.

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• 160738-57-8(Gatifloxacin)
• 114213-69-3(N-Methyl Gatifloxacin)
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• 180200-66-2(Gatifloxacin sesquihydrate)
• 82419-36-1(Ofloxacin)
• 112811-59-3(Gatifloxacin)
• 172426-87-8(Desethylene Gatifloxacin)
• 100986-85-4(Levofloxacin)