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Avermectin chemistry and action: ester- and ether-type candidate photoaffinity probes.

Abstract：

: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 IC50 values of 7-57 nM in competing for the [3H]1 binding site.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tsukamoto Y,Cole LM,Casida JE

doi

10.1016/s0968-0896(99)00259-x

subject

Has Abstract

pub_date

2000-01-01 00:00:00

pages

19-26

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(99)00259-X

journal_volume

8

pub_type

杂志文章

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