Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase

2007 ◽  
Vol 15 (5) ◽  
pp. 2106-2119 ◽  
Author(s):  
João Neres ◽  
Pascal Bonnet ◽  
Philip N. Edwards ◽  
Pravin L. Kotian ◽  
Alejandro Buschiazzo ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Benzoic Acid ◽  
Pyridine Derivatives

Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase

2005 ◽  
Vol 13 (7) ◽  
pp. 2665-2678 ◽  
Author(s):  
Pooran Chand ◽  
Pravin L. Kotian ◽  
Philip E. Morris ◽  
Shanta Bantia ◽  
David A. Walsh ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
Inhibitory Activity ◽  
Pyridine Derivatives

Structure-Based Virtual Screening of New Benzoic Acid Derivatives as Trypanosoma cruzi Trans-sialidase Inhibitors

2020 ◽  
Vol 16 ◽  
Author(s):  
Lenci Karina Vázquez-Jiménez ◽  
Alma Delia Paz-González ◽  
Alfredo Juárez-Saldivar ◽  
María Laura Uhrig ◽  
Rosalía Agusti ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Virtual Screening ◽  
Trypanosoma Cruzi ◽  
Benzoic Acid ◽  
New Agents ◽  
Trypanocidal Activity ◽  
Acetylneuraminic Acid ◽  
Benzoic Acid Derivatives ◽  
Lead Compounds ◽  
Docking Approach

Background: Chagas disease, caused by the parasite Trypanosoma cruzi represents a worldwide epidemiological, economic, and social problem. In the last decades, the trans-sialidase enzyme of Trypanosoma cruzi has been considered an attractive target for the development of new agents with potential trypanocidal activity. Objective: In this work, the aim was find new potential non-sugar trans-sialidase inhibitors using benzoic acid as a scaffold. Method: A structure-based virtual screening of the ZINC15 database was carried out. Additionally, the enzyme and trypanocidal activity of the selected compounds was determined. Results: The results of this work detected 487 compounds derived from benzoic acid as potential trans-sialidase inhibitors with a more promising binding energy value (< -7.7 kcal/mol) than the known inhibitor 2,3-dehydro-2-deoxy-N-acetylneuraminic acid (DANA). In particular, two lead compounds, V1 and V2 turned out to be promising trans-sialidase inhibitors. Even though the trypanocidal activity displayed was low, these compounds showed trans-sialidase inhibition values of 87.6% and 29.6%, respectively. Conclusion: Structure-based virtual screening using a molecular docking approach is a useful method for the identification of new transsialidase inhibitors.

Ouabain-Insensitive Na+-ATPase Activity in Trypanosoma cruzi Epimastigotes

1999 ◽  
Vol 54 (1-2) ◽  
pp. 100-104 ◽  
Author(s):  
Celso Caruso-Neves ◽  
Marcelo Einicker-Lamas ◽  
Carlos Chagas ◽  
Mecia Maria Oliveira ◽  
Adalberto Vieyra ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Benzoic Acid ◽  
Atpase Activity ◽  
Cell Types ◽  
Dependent Manner ◽  
Rectangular Hyperbola ◽  
The Hill ◽  
Dose Dependent ◽  
Hill Number ◽  
Amino Benzoic Acid

In the present paper, the presence of a ouabain-insensitive Na+-stimulated, Mg2+-dependent ATPase activity in T. cruzi epimastigotes CL14 clone and Y strain was investigated. The increase in Na+ concentration (from 5 to 170 mᴍ), in the presence of 2 mᴍ ouabain, increases the ATPase activity in a saturable manner along a rectangular hyperbola. The was 18.0 ± 1.0 and 21.1 ± 1.1 nmoles Pi x mg-1 x min-1 and the half-activation value (K50) for Na+ was 34.3 ± 5.8 mᴍ and 37.7 ± 5.3 in CL14 clone and in Y strain, respectively. The Na+-stimulated ATPase activity was inhibited by 5-[aminosulfonyl]-4-chloro-2-[(2-furanylmethyl)-amino] benzoic acid (furosemide) in a dose-dependent manner. The half-inhibition value (I50) was 0.22 ± 0.03 and 0.24 ± 0.07 mᴍ, and the Hill number (n) was 0.99 ± 0.2 and 2.16 ± 0.29 for CL14 clone and Y strain, respectively. These data indicate that both cell types express the ouabain-insensitive Na+-ATPase activity, which might be considered the bio­chemical expression of the second Na+ pump

Trypanosoma cruzi: Inhibition of Parasite Growth and Respiration by Oxazolo(thiazolo)pyridine Derivatives and Its Relationship to Redox Potential and Lipophilicity

2001 ◽  
Vol 99 (1) ◽  
pp. 1-6 ◽  
Author(s):  
Juan Diego Maya ◽  
Antonio Morello ◽  
Yolanda Repetto ◽  
Andrés Rodrı́guez ◽  
Pilar Puebla ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Redox Potential ◽  
Parasite Growth ◽  
Pyridine Derivatives

TEM characterization of proton-exchanged LiNbO3 optical waveguides

1986 ◽  
Vol 44 ◽  
pp. 480-481
Author(s):  
W. E. Lee
Keyword(s):  
Refractive Index ◽  
Benzoic Acid ◽  
Optical Waveguides ◽  
Total Internal Reflection ◽  
Index Of Refraction ◽  
Optical Measurements ◽  
Lithium Ions ◽  
Wide Channel ◽  
Tem Characterization

An optical waveguide consists of a several-micron wide channel with a slightly different index of refraction than the host substrate; light can be trapped in the channel by total internal reflection.Optical waveguides can be formed from single-crystal LiNbO3 using the proton exhange technique. In this technique, polished specimens are masked with polycrystal1ine chromium in such a way as to leave 3-13 μm wide channels. These are held in benzoic acid at 249°C for 5 minutes allowing protons to exchange for lithium ions within the channels causing an increase in the refractive index of the channel and creating the waveguide. Unfortunately, optical measurements often reveal a loss in waveguiding ability up to several weeks after exchange.

Protective effect of Trypanosoma rangeli against infections with a highly virulent strain of Trypanosoma cruzi

1997 ◽  
Vol 2 (5) ◽  
pp. 482-487 ◽  
Author(s):  
Claudio Zuniga ◽  
Teresa Palau ◽  
Pilar Penin ◽  
Carlos Gamallo ◽  
Jose Antonio de Diego
Keyword(s):  
Trypanosoma Cruzi ◽  
Protective Effect ◽  
Virulent Strain ◽  
Trypanosoma Rangeli ◽  
Highly Virulent
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