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New phenyl thiosulfonate (TSO) targeted covalent inhibitors (TCIs) show promise against Chagas disease. TSO-13 effectively inhibits Cruzipain (CZP) in parasite-infected cells, offering a potential new antichagasic agent.

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Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Chagas disease is a neglected tropical disease with inadequate treatments.
  • Cruzipain (CZP), a cysteine protease from *T. cruzi*, is a validated drug target.
  • Reversible targeted covalent inhibitors (TCIs) are being explored for antichagasic activity.

Purpose of the Study:

  • To design and synthesize novel phenyl thiosulfonate (TSO)-based TCIs.
  • To optimize enzymatic activity and *in vitro* to *in vivo* bioactivity translation.
  • To identify potent and selective inhibitors of *T. cruzi* Cruzipain (CZP).

Main Methods:

  • Synthesis of phenyl TSO derivatives.
  • Enzymatic inhibition assays against CZP and human cathepsin L.
  • Evaluation of bioactivity in *T. cruzi*-infected cell models.
  • Computational studies of inhibitor-target interactions.

Main Results:

  • Ten potent phenyl TSO TCIs were identified.
  • TSO-13 demonstrated high CZP inhibitory potency and selectivity.
  • TSO-13 showed excellent bioactivity translation in infected cells.
  • Computational analysis revealed TSO's role in reactivity and complex stability.

Conclusions:

  • Triazole-based phenyl TSO derivatives are promising for CZP inhibitor design.
  • TSO-13 represents a potential lead compound for novel antichagasic agents.
  • This research contributes to developing innovative treatments for Chagas disease.