Zhang, Yong-Kang published the artcileDiscovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide, Application of 1,3-Dichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(23), 5589-5593, database is CAplus and MEDLINE.
A novel series of isoxazoline benzoxaborole small mols. 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 mol., (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 (t1/2 = 22 days). Compound 38 demonstrated 97.6% therapeutic effectiveness within 24 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 50 mg/kg in dogs.
Bioorganic & Medicinal Chemistry Letters published new progress about 864725-22-4. 864725-22-4 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Alkenyl,Benzene, name is 1,3-Dichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene, and the molecular formula is C10H10O2, Application of 1,3-Dichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene.
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