Antichagasic profile of a Series of Mannich Base‐Type Derivatives: Design, Synthesis, in vitro Evaluation, and Computational Studies Involving Iron Superoxide Dismutase

2019 ◽  
Vol 4 (27) ◽  
pp. 8112-8121
Author(s):  
Rocío Paucar ◽  
Rubén Martín‐Escolano ◽  
Elsa Moreno‐Viguri ◽  
Nuria Cirauqui ◽  
Clotilde Marín ◽  
...  
Keyword(s):  
Superoxide Dismutase ◽  
Mannich Base ◽  
Computational Studies ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Iron Superoxide Dismutase

scholarly journals In vitro antileishmanial activity and iron superoxide dismutase inhibition of arylamine Mannich base derivatives

Parasitology ◽  
2017 ◽  
Vol 144 (13) ◽  
pp. 1783-1790 ◽  
Author(s):  
ALVARO MARTIN-MONTES ◽  
MERY SANTIVAÑEZ-VELIZ ◽  
ELSA MORENO-VIGURI ◽  
RUBÉN MARTÍN-ESCOLANO ◽  
CARMEN JIMÉNEZ-MONTES ◽  
...  
Keyword(s):  
Superoxide Dismutase ◽  
Leishmania Donovani ◽  
Mannich Base ◽  
Neglected Diseases ◽  
Leishmania Braziliensis ◽  
Reference Drug ◽  
Iron Superoxide Dismutase ◽  
Therapeutic Tools

SUMMARYLeishmaniasis is one of the world's most neglected diseases, and it has a worldwide prevalence of 12 million. There are no effective human vaccines for its prevention, and treatment is hampered by outdated drugs. Therefore, research aiming at the development of new therapeutic tools to fight leishmaniasis remains a crucial goal today. With this purpose in mind, we present 20 arylaminoketone derivatives with a very interesting in vitro and in vivo efficacy against Trypanosoma cruzi that have now been studied against promastigote and amastigote forms of Leishmania infantum, Leishmania donovani and Leishmania braziliensis strains. Six out of the 20 Mannich base-type derivatives showed Selectivity Index between 39 and 2337 times higher in the amastigote form than the reference drug glucantime. These six derivatives affected the parasite infectivity rates; the result was lower parasite infectivity rates than glucantime tested at an IC25 dose. In addition, these derivatives were substantially more active against the three Leishmania species tested than glucantime. The mechanism of action of these compounds has been studied, showing a greater alteration in glucose catabolism and leading to greater levels of iron superoxide dismutase inhibition. These molecules could be potential candidates for leishmaniasis chemotherapy.

scholarly journals Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators

2021 ◽  
Vol 36 (1) ◽  
pp. 1370-1377
Author(s):  
Daniel A. S. Kitagawa ◽  
Rafael B. Rodrigues ◽  
Thiago N. Silva ◽  
Wellington V. dos Santos ◽  
Vinicius C. V. da Rocha ◽  
...  
Keyword(s):  
In Silico ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
In Silico Studies ◽  
Acetylcholinesterase Reactivators

Design, Synthesis, and In Vitro Evaluation of Tubulin‐targeting Dibenzothiazines with Antiproliferative Activity as Novel Heterocycle Building Block

ChemMedChem ◽  
2021 ◽  
Author(s):  
Walter Damián Guerra ◽  
Daniel Lucena-Agell ◽  
Rafael Hortigüela ◽  
Roberto Arturo Rossi ◽  
J. Fernando Díaz ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Building Block ◽  
Design Synthesis ◽  
In Vitro Evaluation

scholarly journals Structure-Based Design, Synthesis, and in vitro Evaluation of Bisubstrate Inhibitors for CatecholO-Methyltransferase (COMT)

2000 ◽  
Vol 6 (6) ◽  
pp. 971-982 ◽  
Author(s):  
Birgit Masjost ◽  
Patrick Ballmer ◽  
Edilio Borroni ◽  
Gerhard Zürcher ◽  
Fritz K. Winkler ◽  
...  
Keyword(s):  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Bisubstrate Inhibitors

Design, synthesis and in vitro evaluation on HRPE cells of ascorbic and 6-bromoascorbic acid conjugates with neuroactive molecules

2004 ◽  
Vol 12 (20) ◽  
pp. 5453-5463 ◽  
Author(s):  
Stefano Manfredini ◽  
Silvia Vertuani ◽  
Barbara Pavan ◽  
Federica Vitali ◽  
Martina Scaglianti ◽  
...  
Keyword(s):  
Design Synthesis ◽  
In Vitro Evaluation

Design, synthesis and in vitro evaluation of phenylbenzamidine derivatives as SSRIs

2007 ◽  
Vol 18 (7) ◽  
pp. 814-816 ◽  
Author(s):  
Jing Yang ◽  
Xiaofang Wang ◽  
Hui Wen ◽  
Fang Qin ◽  
Guang Zhong Yang
Keyword(s):  
Design Synthesis ◽  
In Vitro Evaluation

Design, synthesis, in-vitro evaluation and molecular docking studies of novel indole derivatives as inhibitors of SIRT1 and SIRT2

2019 ◽  
Vol 92 ◽  
pp. 103281 ◽  
Author(s):  
Ramu Manjula ◽  
Nikhila Gokhale ◽  
Sruthi Unni ◽  
Prashant Deshmukh ◽  
Rajkumar Reddyrajula ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Studies ◽  
Indole Derivatives ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Molecular Docking Studies

scholarly journals Design, synthesis and in vitro evaluation against human cancer cells of 5-methyl-5-styryl-2,5-dihydrofuran-2-ones, a new series of goniothalamin analogues

2013 ◽  
Vol 21 (17) ◽  
pp. 5107-5117 ◽  
Author(s):  
Marjorie Bruder ◽  
Débora Barbosa Vendramini-Costa ◽  
João Ernesto de Carvalho ◽  
Ronaldo Aloise Pilli
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Human Cancer Cells
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