Avermectin chemistry and action: ester- and ether-type candidate photoaffinity probes.
Avermectin chemistry and action: ester- and ether-type candidate photoaffinity probes.
复制标题
阿维菌素化学和作用：酯型和醚型候选光亲和探针。
DOI：
10.1016/s0968-0896(99)00259-x
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发表时间：
2000
影响因子：
3.5
通讯作者：
Casida,JE
中科院分区：
文献类型：
--
作者：
Tsukamoto,Y;Cole,LM;Casida,JE
阿维菌素B1 a（1）是一种强效驱虫剂、杀虫剂、杀螨剂和氯离子通道激活剂，通过[3 H]1结合试验分析，可与特定神经膜位点相互作用。候选人的光亲和探针制备取代dioleandrosyl取代基与潜在的电子等排的酯和醚接近原始的总原子长度和终止于苯基取代的叠氮基，碘或羟基。几种候选物达到了对小鼠、家蝇和果蝇脑氯离子通道的高效力目标，竞争[3 H]1结合位点的IC 50值为7-57 nM。
Avermectin B1a(1) is a potent anthelmintic, insecticide, miticide and chloride channel activator on interaction with a specific nerve membrane site analyzed by binding assays with [3H]1. Candidate photoaffinity probes were prepared replacing the dioleandrosyl substituent with potential isosteric esters and ethers approximating the original overall atom length and terminating in a phenyl moiety substituted with azido, iodo or hydroxy. Several of the candidates met the goal of high potency on mouse, housefly and fruit fly brain chloride channels with IC50values of 7–57 nM in competing for the [3H]1 binding site.