کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584864 | 981354 | 2015 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 23, 1 December 2015, Pages 5589-5593
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 23, 1 December 2015, Pages 5589-5593
نویسندگان
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,