Novel Triorganotins against Adult and Larval Mosquitoes

针对成蚊和幼虫蚊子的新型三有机锡

• 批准号: 6821281
• 负责人: GEORGE ENG
• 金额: $ 18.06万
• 依托单位: UNIVERSITY OF THE DISTRICT OF COLUMBIA
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-09-01 至 2008-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6821281
• 关键词: Aedes; Anopheles; Culex; chemical structure function; chemical synthesis; disease vectors; drug design /synthesis /production; insect control; insecticide biological effect; insecticides; larva; mature animal; pyrethroid; toxicant screening

The specific goals of this research are to evaluate the effectiveness of triorganotin pyrethroid compounds as potential insecticides against larvae and adults of vector mosquitoes as well as to develop structure-activity relationship(s) between a parameter or parameters of the molecule and their toxicity. One species of mosquitoes to be used is in the genus Anopheles that includes vectors of human malaria parasites. A second species to be studied is Aedes aegypti, the primary vector of dengue and yellow fever. The third species of mosquitoes to be investigated are members of the Culex pipiens group that are responsible for the transmission of West Nile virus. The development of a new class of effective insecticides would be of tremendous value in the effort to reduce the spread of these highly debilitating and sometimes deadly diseases. Triorganotin compounds could potentially overcome problems such as resistance, commonly found with other insecticides. In addition, triorganotins are known to biodegrade to a non-toxic species, SnC14, in the environment. To accomplish these goals, triorganotin pyrethroid compounds will be synthesized and screened for their effectiveness against mosquito larvae and adult female mosquitoes. Initial studies will involve incorporating a triorganotin moiety into fragments of pyrethrins or those that mimic components of pyrethrin that have shown insecticidal activity. Long-term effects of the compounds will be evaluated using residual and delayed studies on the mosquito larvae. The insecticidal activity against adult mosquitoes on representative housing construction materials such as concrete, will also be evaluated. After evaluating the results of these studies, new triorganotin compounds will be designed and synthesized with the aim of developing more effective compounds. To reduce the number of compounds that must be synthesized and tested, quantitative structure-activity relationships (QSARs) between a physical parameter or parameters of the triorganotins and their toxicity will be developed.

本研究的具体目标是评价三有机锡拟除虫菊酯的有效性 化合物作为针对媒介蚊子的幼虫和成虫的潜在杀虫剂以及开发分子的一个或多个参数与其毒性之间的结构-活性关系。待使用的一种蚊子是包括人类疟疾寄生虫载体的按蚊属。 第二个要研究的物种是埃及伊蚊，它是登革热和黄热病的主要媒介。第三种待调查的蚊子是负责传播西尼罗河病毒的尖音库蚊。开发一类新的有效杀虫剂将对减少这些高度致弱和有时致命的疾病的传播具有巨大价值。三有机锡化合物有可能克服其他杀虫剂常见的抗药性等问题。此外，已知三有机锡在环境中可生物降解为无毒物质SnC 14。为了实现这些目标，将合成三有机锡拟除虫菊酯化合物，并筛选其对蚊子幼虫和成年雌蚊的有效性。初步研究将 包括将三有机锡部分掺入到除虫菊酯片段中或掺入到已显示出杀虫活性的除虫菊酯的模拟组分中。将通过对蚊子幼虫的残留和延迟研究来评估化合物的长期影响。还将评估对代表性住房建筑材料（如混凝土）上的成蚊的杀虫活性。在评估这些研究结果之后，将设计和合成新的三有机锡化合物，目的是开发更有效的化合物。为了减少必须合成的化合物的数量， 通过测试，将开发三有机锡的一个或多个物理参数与其毒性之间的定量结构-活性关系（QSAR）。