Potency and selectivity of trifluoroacetylimino and pyrazinoylimino nicotinic insecticides and their fit at a unique binding site niche.
Potency and selectivity of trifluoroacetylimino and pyrazinoylimino nicotinic insecticides and their fit at a unique binding site niche.
复制标题
三氟乙酰亚氨基和吡嗪酰亚氨基烟碱类杀虫剂的效力和选择性及其在独特结合位点生态位的适合性。
DOI：
10.1021/jm800191a
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发表时间：
2008
影响因子：
7.3
通讯作者：
Casida,JohnE
中科院分区：
文献类型：
--
作者：
Tomizawa,Motohiro;Kagabu,Shinzo;Ohno,Ikuya;Durkin,KathleenA;Casida,JohnE
Neonicotinoid agonists with a nitroimino or cyanoimino pharmacophore are the newest of the four most important classes of insecticides. Our studies on the nicotinic receptor structure in the neonicotinoid-bound state revealed a unique niche of about 6 Å depth beyond the nitro oxygen or cyano nitrogen tip. The N-substituted imino pharmacophore was therefore extended to fill the gap. Excellent target site selectivity with high insecticidal activity and low toxicity to mammals were achieved rivaling those of the current neonicotinoid insecticides as illustrated here by 3-(6-chloropyridin-3-ylmethyl)-2-trifluoroacetyliminothiazoline and its pyrazinoylimino analogue.
