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

Autor: Muhammad Kashif, Antonio Moreno-Herrera, Juan Carlos Villalobos-Rocha, Benjamín Nogueda-Torres, Jaime Pérez-Villanueva, Karen Rodríguez-Villar, José Lius Medina-Franco, Peterson de Andrade, Ivone Carvalho, Gildardo Rivera
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Molecules, Vol 22, Iss 11, p 1863 (2017)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules22111863
Popis: Chagas, or American trypanosomiasis, remains an important public health problem in developing countries. In the last decade, trans-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 trans-sialidase (TS) inhibitors and anti-trypanosomal agents. Three compounds (14, 18, and 19) sharing a para-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 (LC50) was
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