ArticleJournal of medicinal chemistry2012
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Synthesis, Antifungal Activity and Molecular Docking Studies of Novel 2-Acyloxybenzamides.Molecules (Basel, Switzerland) · 2026Article
- Application of Data-Centric Supervised Machine Learning to Predict Phenotypic Activity Against Clinically Relevant Stages ofPharmaceutics · 2025Article
- Naphthyl bearing 1,3,4-thiadiazoleacetamides targeting the parasitic folate pathway as anti-infectious agents:RSC medicinal chemistry · 2023Article
- Mesoporous Carbon-Supported Pd Nanoparticles in the Metallic State-Catalyzed Acylation of Amides with Aryl Esters via C-O Activation.ACS omega · 2022Article
- Chemical Characterization and Biological Evaluation of New Cobalt(II) Complexes with Bioactive Ligands, 2-Picolinehydroxamic Acid and Reduced Schiff BasePharmaceuticals (Basel, Switzerland) · 2021Article
- Equilibria in Aqueous Cobalt(II)-Reduced Schiff BaseMolecules (Basel, Switzerland) · 2020Article
- Intramolecular Hydrogen Bonding Involving Organic Fluorine: NMR Investigations Corroborated by DFT-Based Theoretical Calculations.Molecules (Basel, Switzerland) · 2017Review
- Review of Experimental Compounds Demonstrating Anti-Toxoplasma Activity.Antimicrobial agents and chemotherapy · 2016Review
- Novel Heteroaryl Selenocyanates and Diselenides as Potent Antileishmanial Agents.Antimicrobial agents and chemotherapy · 2016Article
- Hybrids of salicylalkylamides and Mannich bases: control of the amide conformation by hydrogen bonding in solution and in the solid state.Molecules (Basel, Switzerland) · 2015Article
- Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.Chemical reviews · 2014Review
- Synthesis Characterization and Antibacterial, Antifungal Activity of N-(Benzyl Carbamoyl or Carbamothioyl)-2-hydroxy Substituted Benzamide and 2-Benzyl Amino-Substituted Benzoxazines.International journal of medicinal chemistry · 2013Article
- Novel N-benzoyl-2-hydroxybenzamide disrupts unique parasite secretory pathway.Antimicrobial agents and chemotherapy · 2012Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
In our efforts to identify novel chemical scaffolds for the development of new antiprotozoal drugs, a compound library was screened against Toxoplasma gondii tachyzoites with activity discovered for N-(4-ethylbenzoyl)-2-hydroxybenzamide 1a against T. gondii as described elsewhere. Synthesis of a compound set was guided by T. gondii SAR with 1r found to be superior for T. gondii , also active against Thai and Sierra Leone strains of Plasmodium falciparum , and with superior ADMET properties as described elsewhere. Herein, synthesis methods and details of the chemical analysis of the compounds in this series are described. Further, this series of N-benzoyl-2-hydroxybenzamides was repurposed for testing against four other protozoan parasites: Trypanosoma brucei rhodesiense , Trypanosoma cruzi , Leishmania donovani , and P. falciparum (K1 isolate). Structure-activity analyses led to the identification of compounds in this set with excellent antileishmanial activity (compound 1d). Overall, compound 1r was the best and had activity 21-fold superior to that of the standard antimalarial drug chloroquine against the K1 P. falciparum isolate.
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