Benzoic Acid Derivatives with Trypanocidal Activity: Enzymatic Analysis and Molecular Docking Studies toward Trans-Sialidase
AbstractChagas, 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 <0.15 µM on the NINOA strain, and LC50 < 0.22 µM on the INC-5 strain. Additionally, compound 18 showed a moderate inhibition (47%) on the trans-sialidase enzyme and a binding model similar to DANA (pattern A). View Full-Text
- Supplementary File 1:
Supplementary (PDF, 211 KB)
Scifeed alert for new publicationsNever miss any articles matching your research from any publisher
- Get alerts for new papers matching your research
- Find out the new papers from selected authors
- Updated daily for 49'000+ journals and 6000+ publishers
- Define your Scifeed now
Kashif, M.; Moreno-Herrera, A.; Villalobos-Rocha, J.C.; Nogueda-Torres, B.; Pérez-Villanueva, J.; Rodríguez-Villar, K.; Medina-Franco, J.L.; de Andrade, P.; Carvalho, I.; Rivera, G. Benzoic Acid Derivatives with Trypanocidal Activity: Enzymatic Analysis and Molecular Docking Studies toward Trans-Sialidase. Molecules 2017, 22, 1863.
Kashif M, Moreno-Herrera A, Villalobos-Rocha JC, Nogueda-Torres B, Pérez-Villanueva J, Rodríguez-Villar K, Medina-Franco JL, de Andrade P, Carvalho I, Rivera G. Benzoic Acid Derivatives with Trypanocidal Activity: Enzymatic Analysis and Molecular Docking Studies toward Trans-Sialidase. Molecules. 2017; 22(11):1863.Chicago/Turabian Style
Kashif, Muhammad; Moreno-Herrera, Antonio; Villalobos-Rocha, Juan C.; Nogueda-Torres, Benjamín; Pérez-Villanueva, Jaime; Rodríguez-Villar, Karen; Medina-Franco, José L.; de Andrade, Peterson; Carvalho, Ivone; Rivera, Gildardo. 2017. "Benzoic Acid Derivatives with Trypanocidal Activity: Enzymatic Analysis and Molecular Docking Studies toward Trans-Sialidase." Molecules 22, no. 11: 1863.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.