1539-06-6Relevant articles and documents
Benzoic acid derivatives with trypanocidal activity: Enzymatic analysis and molecular docking studies toward trans-sialidase
Kashif, Muhammad,Moreno-Herrera, Antonio,Villalobos-Rocha, Juan Carlos,Nogueda-Torres, Benjamín,Pérez-Villanueva, Jaime,Rodríguez-Villar, Karen,Medina-Franco, José Luis,De Andrade, Peterson,Carvalho, Ivone,Rivera, Gildardo
, (2017)
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 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).
DERIVATIVES OF 5(6)-BENZIMIDAZOLECARBOXYLIC ACID
Sklyarova, I. V.,Garabadzhiu, A. V.,Ginzburg, O. F.
, p. 578 - 582 (2007/10/02)
2-Aryl-5(6)-benzimidazolecarboxamides containing a 3-dimethylaminopropyl or 5-carboxypentyl group in the carboxamide fragment were synthesized by the condensation of the methoxyethylimidic esters of aromatic acids with o-diamines.
Synthesis of indophenazines and 6-piperidino/morpholino-methylindophenazines as possible excystment and cysticidal agents
Varma,Khan
, p. 1043 - 1045 (2007/10/05)
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