Synthesis, characterization and utilization of a new series of 1,2,3-triazole derivatives to neutralize some toxic activities of Bothrops jararaca snake venom
Braz. J. Pharm. Sci. (Online)
; 58: e201143, 2022. tab, graf
Article
en En
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LILACS-Express
| LILACS
| ID: biblio-1420361
Biblioteca responsable:
BR1.1
ABSTRACT
Abstract Snake envenomation is a public health problem, and while serum therapy prevents death, the local effects of venoms can lead to amputations or morbidities. Thus, alternative treatments deserve attention. In this study, we tested eight derivatives of 1,2,3-triazole against some toxic activities of Bothrops jararaca venom. The derivatives were synthesized, and their structures analyzed by infrared and nuclear magnetic resonance. After that, the ability of compounds to inhibit hemolysis, coagulation, proteolysis, hemorrhaging, edema, and lethal activities of B. jararaca venom was investigated. The derivatives were incubated with B. jararaca venom (incubation protocol), administered before (prevention protocol) or after (treatment protocol) injecting venom into the mice. Then, hemorrhaging assay occurred. As a result, most of the derivatives inhibited the activities, even if they were incubated, injected before or after B. jararaca venom. However, the derivatives TRI 07 and TRI 18 seemed to be the most efficient in impairing hemorrhaging. The derivatives showed a low drug score of toxicity based on an in silico technique. Therefore, the derivatives fulfilled physicochemical and biological requirements to become drugs, and they may be a brand new initiative for designing antivenom molecules to complement antivenom therapy to efficiently block tissue necrosis or any other local effects.
Texto completo:
1
Colección:
01-internacional
Base de datos:
LILACS
Tipo de estudio:
Guideline
Idioma:
En
Revista:
BJPS
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Braz. J. Pharm. Sci. (Impr.)
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Braz. J. Pharm. Sci. (Online)
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Braz. j. pharm. sci. (Online)
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Brazilian Journal of Pharmaceutical Sciences (Impresso)
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Brazilian Journal of Pharmaceutical Sciences (Online)
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Brazilian journal of pharmaceutical sciences (Impresso)
Asunto de la revista:
Farmacologia
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Teraputica
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Toxicologia
Año:
2022
Tipo del documento:
Article
País de afiliación:
Brasil
Pais de publicación:
Brasil