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Side Chain-Modified Benzothiazinone Derivatives with Anti-Mycobacterial Activity.

Dongguang Fan1, Bin Wang2, Giovanni Stelitano3

  • 1College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China.

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|July 29, 2023
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Summary
This summary is machine-generated.

New benzothiazinone (BTZ) analogues combat tuberculosis (TB) by inhibiting Mycobacterium tuberculosis (Mtb) DprE1. Compound 37 shows improved solubility and bioavailability, demonstrating efficacy in mouse models for this infectious disease.

Keywords:
DprE1 inhibitoranti-tubercular agentsin vivo activitystructure activity relationship

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Area of Science:

  • Medicinal Chemistry
  • Microbiology
  • Drug Discovery

Background:

  • Tuberculosis (TB) remains a critical global health challenge, exacerbated by rising antibiotic resistance.
  • The benzothiazinone (BTZ) scaffold, exemplified by PBTZ169, targets the essential enzyme decaprenylphosphoryl-β-D-ribose 2'-oxidase (DprE1) in Mycobacterium tuberculosis (Mtb).
  • Existing BTZ inhibitors suffer from poor aqueous solubility, limiting their drug-like properties and therapeutic potential.

Purpose of the Study:

  • To design and synthesize novel BTZ analogues with improved physicochemical properties.
  • To identify potent DprE1 inhibitors with enhanced solubility and bioavailability for TB treatment.
  • To evaluate the in vitro and in vivo efficacy of optimized BTZ compounds against Mtb.

Main Methods:

  • Systematic modification of the BTZ scaffold to generate a library of analogues.
  • Determination of minimum inhibitory concentrations (MIC) against Mtb.
  • Assessment of aqueous solubility and in vivo pharmacokinetic parameters (bioavailability).
  • Evaluation of anti-TB activity in a murine infection model.

Main Results:

  • Several synthesized BTZ analogues exhibited potent antimycobacterial activity, with MIC values below 0.01 µM.
  • Compound 37 demonstrated significantly improved aqueous solubility and bioavailability compared to the parent compound PBTZ169.
  • Compound 37 effectively reduced Mtb burden in a mouse model of acute TB infection.

Conclusions:

  • Novel BTZ analogues offer a promising avenue for developing new anti-TB drugs.
  • Compound 37 represents a lead candidate with enhanced drug-like properties and demonstrated in vivo efficacy.
  • Further development of these optimized BTZ compounds could address the urgent need for effective TB therapeutics.