Study on the synthesis and structure-activity relationship of 1,2,3-triazoles against toxic activities of Bothrops jararaca venom.

Zeitschrift fur Naturforschung. C, Journal of biosciences(2022)

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摘要
Snakebite envenoming is a health concern and has been a neglected tropical disease since 2017, according to the World Health Organization. In this study, we evaluated the ability of ten 1,2,3-triazole derivatives AM001 to AM010 to inhibit pertinent (coagulant, hemolytic, and proteolytic) and (hemorrhagic, edematogenic, and lethal) activities of venom. The derivatives were synthesized, and had their molecular structures fully characterized by CHN element analysis, Fourier-transform infrared spectroscopy and Nuclear magnetic resonance. The derivatives were incubated with the  venom (incubation protocol) or administered before (prevention protocol) or after (treatment protocol) the injection of venom into the animals. Briefly, the derivatives were able to inhibit the main toxic effects triggered by venom, though with varying efficacies, and they were devoid of toxicity through , or analyses. However, it seemed that the derivatives AM006 or AM010 inhibited more efficiently hemorrhage or lethality, respectively. The derivatives were nontoxic. Therefore, the 1,2,3-triazole derivatives may be useful as an adjuvant to more efficiently treat the local toxic effects caused by envenoming.
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关键词
Bothrops jararaca ,1,2,3-triazole derivatives,antivenom,medicinal chemistry,snake venom
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