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新型甘油-氟代三唑衍生物的合成及其植物毒性和细胞遗传毒性评价。

Synthesis of novel glycerol-fluorinated triazole derivatives and evaluation of their phytotoxic and cytogenotoxic activities.

机构信息

Universidade Vila Velha, Programa de Pós-graduação em Biotecnologia Vegetal, Rua José Dantas de Melo, 21, Boa Vista, 29102-770 Vila Velha, ES, Brazil.

Universidade Federal do Espírito Santo, Departamento de Biologia, Alto Universitário, s/n, Guararema, 29500-000 Alegre, ES, Brazil.

出版信息

An Acad Bras Cienc. 2023 Mar 13;95(1):e20211102. doi: 10.1590/0001-3765202320211102. eCollection 2023.

DOI:10.1590/0001-3765202320211102
PMID:36946806
Abstract

The control of weeds in agriculture is mainly conducted with the use of synthetic herbicides. However, environmental and human health concerns and increased resistance of weeds to existing herbicides have increased the pressure on researchers to find new active ingredients for weed control which present low toxicity to non-target organisms, are environmentally safe, and can be applied at low concentrations. It is herein described the synthesis of glycerol-fluorinated triazole derivatives and evaluation of their phytotoxic and cytogenotoxic activities. Starting from glycerol, ten fluorinated triazole derivatives were prepared in four steps. The assessment of them on Lactuca sativa revealed that they present effects on phytotoxic and cytogenotoxic parameters with different degrees of efficiency. The compounds 4a, 4b, 4d, 4e, 4i, and 4j have pre-emergent inhibition behavior, while all the investigated compounds showed post emergent effect. Mechanism of action as clastogenic, aneugenic, and epigenetic were observed in the lettuce root meristematic cells, with alterations as stick chromosome, bridge, delay, c-metaphase, and loss. It is believed that glycerol-fluorinated triazole derivatives possess a scaffold that can be explored towards the development of new chemicals for the control of weed species.

摘要

农业杂草的防治主要采用合成除草剂。然而,由于对环境和人类健康的关注以及杂草对现有除草剂的抗药性增加,研究人员面临着寻找新的除草活性成分的压力,这些成分对非靶标生物的毒性低、对环境安全,并且可以低浓度使用。本文描述了甘油-氟代三唑衍生物的合成及其除草和细胞遗传毒性活性的评价。从甘油出发,经过四步反应合成了 10 个氟代三唑衍生物。对莴苣的评估表明,它们对植物毒性和细胞遗传毒性参数具有不同程度的影响。化合物 4a、4b、4d、4e、4i 和 4j 具有早期抑制作用,而所有研究的化合物都表现出后期效应。在生菜根尖分生细胞中观察到了致裂、变倍和表观遗传作用,表现为着丝粒染色体、桥、延迟、中期 c 和丢失。相信甘油-氟代三唑衍生物具有可以开发用于防治杂草的新化学物质的结构。

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