Related Experiment Video

Updated: Jul 24, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.2K

1-hydroxy-7-azabenzotriazole-cinnamic esters as anti-Toxoplasma gondii agents

Xinyue Liu1, Weifeng Yan2, Guang Yang3

  • 1Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University, Yanji, China.

Natural Product Research
|May 8, 2025
PubMed

Insights

New cinnamic ester derivatives show potent activity against Toxoplasma gondii. This research offers promising drug candidates for treating toxoplasmosis, a significant global health concern.

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Conventional chemotherapy for toxoplasmosis faces challenges due to drug resistance and toxicity.
  • Targeted therapeutics with improved safety and efficacy are needed to combat Toxoplasma gondii infections.
  • Developing novel anti-parasitic agents is crucial for reducing the global burden of toxoplasmosis.

Purpose of the Study:

  • To synthesize and evaluate novel 1-hydroxy-7-azabenzotrexate-cinnamic esters as potential anti-Toxoplasma gondii agents.
  • To investigate the structure-activity relationships of these compounds against T. gondii.
  • To explore efficient synthesis methods for these promising drug candidates.

Main Methods:

  • A one-step synthesis method was developed for 1-hydroxy-7-azabenzotrexate-cinnamic esters.
  • Structure-activity relationship (SAR) analysis was performed to identify key structural features for anti-T. gondii activity.
  • The biological activity of synthesized compounds was assessed against T. gondii.

Main Results:

  • The synthesis of 1-hydroxy-7-azabenzotrexate-cinnamic esters was successfully demonstrated.
  • The compound 3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl (E)-3-(3,4,5-trifluorophenyl)acrylate (12), featuring a 3,4,5-trifluorophenyl group, exhibited significantly enhanced activity against T. gondii.
  • SAR analysis confirmed the crucial role of the trifluorophenyl moiety in augmenting anti-T. gondii efficacy.

Conclusions:

  • 1-hydroxy-7-azabenzotrexate-cinnamic esters represent a promising class of compounds for the development of novel anti-Toxoplasma gondii therapeutics.
  • The identified lead compound (12) warrants further investigation for its potential as an anti-toxoplasmosis drug.
  • This study contributes to the ongoing efforts to find effective treatments for toxoplasmosis.
Keywords:
1-hydroxy-7-azabenzotriazole-cinnamic acid estersToxoplasma gondiianti-T. gondii agentsstructure-function relationship

More Related Videos

Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions07:12

Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions

Published on: July 17, 2020

6.2K
Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine11:04

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine

Published on: June 13, 2022

2.9K

Related Concept Videos

Toxoplasmosis01:28

Toxoplasmosis

Toxoplasmosis, a zoonotic disease caused by the protozoan Toxoplasma gondii, poses significant public health challenges globally due to its high seroprevalence and varied clinical manifestations. As an obligate intracellular parasite, T. gondii can infect all warm-blooded vertebrates, but felids are its only definitive hosts, shedding unsporulated oocysts into the environment. Humans typically acquire the infection through ingestion of tissue cysts in undercooked meat or oocysts from...
Anthelminthic Agents01:15

Anthelminthic Agents

Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
Antiprotozoal Agents01:21

Antiprotozoal Agents

Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...