- Synthesis and antiplasmodial assessment of nitazoxanide and analogs as new antimalarial candidates
-
During the last years, the progression to control malaria disease seems to be slowed and WHO (World Health Organization) reported a modeling analysis with the prediction of the increase in malaria morbidity and mortality in sub-Saharan Africa during the COVID-19 pandemic. A rapid way to the discovery of new drugs could be carried out by performing investigations to identify drugs based on repurposing of “old” drugs. The 5-nitrothiazole drug, Nitazoxanide was shown to be active against intestinal protozoa, human helminths, anaerobic bacteria, viruses, etc. In this work, Nitazoxanide and analogs were prepared using two methodologies and evaluated against P. falciparum 3D7. A bithiazole analog, showed attractive inhibitory activity with an EC50 value of 5.9 μM, low propensity to show toxic effect against HepG2 cells at 25 μM, and no cross-resistance with standard antimalarials.
- Aguiar, Anna Caroline Campos,Guido, Rafael Victorio Carvalho,Irabuena, Camila,Mendes, Giovana Rossi,Scarone, Laura,Serra, Gloria,de Souza, Guilherme Eduardo
-
-
- Thiazole compound as well as preparation method and application thereof
-
The invention relates to thiazole compounds as well as a preparation method and application thereof, and belongs to the field of medicinal chemistry. The compound has a structural general formula described in the specifications of the invention; the compound or the prodrug thereof or pharmaceutically acceptable salts of the compound not only can significantly improve the biological activity, but also can effectively reduce the loss of biological activity due to glycosylation, significantly improve the exposure of effective drugs, and can be used for preparing medicines for preventing or treating hepatic fibrosis, medicines for preventing or treating viral influenza, medicines for treating Alzheimer's disease and Parkinson's disease and the like, and the clinical application of the compound is expanded.
- -
-
Paragraph 0117-0119; 0121-0123
(2021/08/21)
-
- Silver(I)-Promoted ipso-Nitration of Carboxylic Acids by Nitronium Tetrafluoroborate
-
A novel and efficient method for the regioselective nitration of a series of aliphatic and aromatic carboxylic acids to their corresponding nitro compounds using nitronium tetrafluoroborate and silver carbonate in dimethylacetamide has been described. This transformation is believed to proceed via the alkyl-silver or aryl-silver intermediate, which subsequently reacts with the nitronium ion to form nitro substances. Mild reaction conditions, tolerant of a broad range of functional groups, and formation of only the ipso-nitrated products are the key features of this methodology when compared to known methods for syntheses of nitroalkyls and nitroarenes.
- Natarajan, Palani,Chaudhary, Renu,Venugopalan, Paloth
-
p. 10498 - 10504
(2015/11/18)
-
