Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10584864 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
Abstract
A novel series of isoxazoline benzoxaborole small molecules was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the ectoparasiticide activity against ticks and fleas. The study identified an orally bioavailable molecule, (S)-3,3-dimethyl-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)benzo[c][1,2]oxaborol-1(3H)-ol (38, AN8030), which was long lasting in dogs (t1/2Â =Â 22Â days). Compound 38 demonstrated 97.6% therapeutic effectiveness within 24Â h of treatment, with residual efficacy of 95.3% against American dog ticks (Dermacentor variabilis) on day 30 and 100% against cat fleas (Ctenocephalides felis) on day 32 after a single oral dose at 50Â mg/kg in dogs.101
Related Topics
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Authors
Yong-Kang Zhang, Jacob J. Plattner, Eric E. Easom, Yasheen Zhou, Tsutomu Akama, Wei Bu, W. Hunter White, Jean M. Defauw, Joseph R. Winkle, Terry W. Balko, Shenghai Guo, Jian Xue, Jianxin Cao, Wuxin Zou,