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An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
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An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity

Published on: November 2, 2016

Ivermectin-derived leishmanicidal compounds.

Anderson Rouge dos Santos1, Camila Alves Bandeira Falcão, Michelle Frazão Muzitano

  • 1Instituto de Química, Universidade Federal do Rio de Janeiro, Ilha do Fundão, CT, Bloco A, CEP 21941-909, Rio de Janeiro, RJ, Brazil.

Bioorganic & Medicinal Chemistry
|December 31, 2008
PubMed
Summary
This summary is machine-generated.

Novel avermectin analogues show potent antileishmanial activity, with conjugated forms and specific subunits outperforming the parent compound, Ivermectin. These derivatives exhibit low toxicity, offering promising leads for treating leishmaniasis.

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A Parasite Rescue and Transformation Assay for Antileishmanial Screening Against Intracellular Leishmania donovani Amastigotes in THP1 Human Acute Monocytic Leukemia Cell Line
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Published on: December 30, 2012

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Leishmaniasis remains a significant global health concern, necessitating novel therapeutic agents.
  • Avermectins, including Ivermectin, are broad-spectrum antiparasitic drugs with potential for repurposing.
  • Understanding structure-activity relationships is crucial for developing effective avermectin-based antileishmanial drugs.

Purpose of the Study:

  • To synthesize and evaluate macrocyclic, acyclic, and seco-analogues of avermectins for antileishmanial activity.
  • To investigate the structural requirements for leishmanicidal activity within the avermectin scaffold.
  • To assess the toxicity profile of novel avermectin analogues.

Main Methods:

  • Synthesis of avermectin analogues from commercial Ivermectin.
  • Assay of antileishmanial activity against axenic promastigote and intracellular amastigote forms of Leishmania amazonensis.
  • Evaluation of compound toxicity.

Main Results:

  • Conjugated Delta(2,3)-Ivermectin (IVM) and its secoester analogues demonstrated enhanced anti-leishmania activity compared to the parent compound.
  • The integrity of the non-conjugated Delta(3,4)-hexahydrobenzofuran moiety is not essential for leishmanicidal activity.
  • The diglycosylated northern subunit showed comparable anti-amastigote potential to the southern hexahydrobenzofuran subunit.
  • Most novel analogues exhibited low toxicity.

Conclusions:

  • Avermectin analogues, particularly conjugated forms and specific subunits, represent promising candidates for antileishmanial drug development.
  • Structural modifications can enhance the efficacy of avermectins against Leishmania parasites.
  • The low toxicity profile of these analogues supports their further investigation as potential therapeutics for leishmaniasis.