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Antitubercular Triazines: Optimization and Intrabacterial Metabolism.

Xin Wang1, Daigo Inoyama1, Riccardo Russo2

  • 1Department of Pharmacology, Physiology and Neuroscience, Rutgers University - New Jersey Medical School, Newark, NJ 07103, USA.

Cell Chemical Biology
|November 13, 2019
PubMed
Summary
This summary is machine-generated.

The novel antitubercular drug JSF-2019 shows potent in vitro efficacy by releasing nitric oxide (NO•) and inhibiting the InhA enzyme. Its improved derivative, JSF-2513, offers better pharmacokinetics for tuberculosis treatment.

Keywords:
Bayesian modelsMycobacterium tuberculosisintrabacterial drug metabolismnitrofurantriazine

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Area of Science:

  • Medicinal Chemistry
  • Microbiology
  • Drug Discovery

Background:

  • JSF-2019 is a triazine antitubercular agent with in vitro efficacy, sharing a nitro group with clinically used drugs.
  • Its activation requires F420H2, nitroreductases, and Ddn, indicating a complex metabolic pathway.

Purpose of the Study:

  • To investigate the activation mechanism and metabolism of JSF-2019 using an intrabacterial drug metabolism (IBDM) platform.
  • To elucidate the structure-activity relationships (SAR) for JSF-2019, leading to improved drug candidates.
  • To determine the combined mechanism of action involving nitric oxide (NO•) release and enzyme inhibition.

Main Methods:

  • Utilized an intrabacterial drug metabolism (IBDM) platform to study drug kinetics and metabolite formation.
  • Conducted structure-activity relationship (SAR) studies to optimize solubility and pharmacokinetic profiles.
  • Performed mechanistic studies with JSF-2019, JSF-2513, and related triazines to identify key biological targets.

Main Results:

  • Demonstrated JSF-2019 activation via F420H2 and nitroreductases, yielding NO• and a des-nitro metabolite.
  • Identified JSF-2513 as an improved analog with enhanced solubility and mouse pharmacokinetics.
  • Established that potent in vitro efficacy is achieved through NO• release and inhibition of InhA and the FAS-II pathway.

Conclusions:

  • The study highlights the critical role of intrabacterial drug metabolism (IBDM) in understanding drug mechanisms.
  • The combined mechanism of NO• release and InhA inhibition is crucial for the antitubercular activity of these triazines.
  • JSF-2513 represents a promising lead compound for further development in tuberculosis therapy.