2. Academic Validation
  3. Cinnamoyl aryl hydrazones as potent leishmanicidal agents: design, synthesis, and structure-activity relationships

Cinnamoyl aryl hydrazones as potent leishmanicidal agents: design, synthesis, and structure-activity relationships

  • Bioorg Med Chem Lett. 2026 Apr:133:130523. doi: 10.1016/j.bmcl.2025.130523.
Renan Augusto Gomes 1,  Leonardo Luiz Gomes Ferreira 2,  Witor Ribeiro Ferraz 3,  Rodrigo Alves Heleno 3,  Fernando Moura Gatti 3,  Mariana Laureano de Souza 2,  Cleydson Breno Rodrigues Dos Santos 4,  Adriano Defini Andricopulo 2,  Gustavo Henrique Goulart Trossini 5
Affiliations

Affiliations

  • 1 LITEC, Department of Pharmacy, School of Pharmaceutical Science, University of São Paulo, 05508-9000, Brazil. Electronic address: renan2.gomes@alumni.usp.br.
  • 2 Laboratory of Medicinal and Computational Chemistry (LQMC), Physics Institute of Sao Carlos, University of São Paulo (USP), São Carlos, SP, Brazil.
  • 3 LITEC, Department of Pharmacy, School of Pharmaceutical Science, University of São Paulo, 05508-9000, Brazil.
  • 4 Postgraduate Program in Biotechnology and Biodiversity-Network BIONORTE, Macapá 68902-280, Amapá, Amazon, Brazil.
  • 5 LITEC, Department of Pharmacy, School of Pharmaceutical Science, University of São Paulo, 05508-9000, Brazil. Electronic address: trossini@usp.br.
PMID: 41453692 DOI: 10.1016/j.bmcl.2025.130523
Abstract

Parasitic diseases like leishmaniasis and Chagas pose significant global health challenges due to limited treatment options and drug resistance. In this study, a series of novel cinnamoyl aryl hydrazone derivatives was synthesized and tested against Leishmania donovani and Trypanosoma cruzi. Four compounds showed promising antileishmanial activity (from 1.27 to 19.53 μM), with two analogues displaying superior potency compared to some current first-line treatments, such as sodium stibogluconate and paromomycin. Computational analyses revealed that activity is driven by specific electronic properties rather than steric factors, while a methyl group consistently reduced potency. The compounds demonstrated favorable predicted ADME properties and were not flagged as aggregators. This research identifies cinnamoyl aryl hydrazones as a promising scaffold for leishmanicidal drug discovery, providing a rational basis for future optimization efforts.

Keywords

Cinnamoyl aryl hydrazones; Computational chemistry; Leishmania donovani; Ligand-based drug design; Tropical neglected disease.

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