Benzoic Acid Derivatives with Trypanocidal Activity: Enzymatic Analysis and Molecular Docking Studies toward Trans-Sialidase

Chagas, or American trypanosomiasis, remains an important public health problem in developing countries. In the last decade, -sialidase has become a pharmacological target for new anti-Chagas drugs. In this work, the aims were to design and find a new series of benzoic acid derivatives as -sialidase...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2017-10, Vol.22 (11), p.1863
Main Authors: Kashif, Muhammad, Moreno-Herrera, Antonio, Villalobos-Rocha, Juan Carlos, Nogueda-Torres, Benjamín, Pérez-Villanueva, Jaime, Rodríguez-Villar, Karen, Medina-Franco, José Lius, de Andrade, Peterson, Carvalho, Ivone, Rivera, Gildardo
Format: Article
Language:English
Subjects:
Amino acids
Animals
Benznidazole
Benzoates - chemical synthesis
Benzoates - chemistry
Benzoates - pharmacology
Benzoic acid
Bioinformatics
Catalysis
Chagas disease
Chemotherapy
Chronic illnesses
Developing countries
docking
Drug Design
Drug development
Drugs
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Enzymes
Glycoproteins - antagonists & inhibitors
Glycoproteins - chemistry
Hydrogen
Immune system
Influenza
inhibitors
LDCs
Lysis
Mice
Models, Molecular
Molecular docking
Molecular Docking Simulation
Molecular Structure
Neuraminidase - antagonists & inhibitors
Neuraminidase - chemistry
Nifurtimox
para-Aminobenzoic acid
Parasites
Pharmacology
Public health
Structure-Activity Relationship
trans-Sialidase
Trypanocidal Agents - chemical synthesis
Trypanocidal Agents - chemistry
Trypanocidal Agents - pharmacology
Trypanosoma cruzi - drug effects
Trypanosomiasis
Vector-borne diseases
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Summary:Chagas, or American trypanosomiasis, remains an important public health problem in developing countries. In the last decade, -sialidase has become a pharmacological target for new anti-Chagas drugs. In this work, the aims were to design and find a new series of benzoic acid derivatives as -sialidase (TS) inhibitors and anti-trypanosomal agents. Three compounds ( , , and ) sharing a -aminobenzoic acid moiety showed more potent trypanocidal activity than the commercially available drugs nifurtimox and benznidazole in both strains: the lysis concentration of 50% of the population (LC ) was
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules22111863