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Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide.
Zhang, Yong-Kang; Plattner, Jacob J; Easom, Eric E; Zhou, Yasheen; Akama, Tsutomu; Bu, Wei; White, W Hunter; Defauw, Jean M; Winkle, Joseph R; Balko, Terry W; Guo, Shenghai; Xue, Jian; Cao, Jianxin; Zou, Wuxin.
Afiliación
  • Zhang YK; Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
  • Plattner JJ; Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
  • Easom EE; Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
  • Zhou Y; Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
  • Akama T; Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
  • Bu W; Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
  • White WH; Elanco Animal Health Research and Development, A Division of Eli Lilly & Company, 2500 Innovation Way, Greenfield, IN 46140, USA.
  • Defauw JM; Elanco Animal Health Research and Development, A Division of Eli Lilly & Company, 2500 Innovation Way, Greenfield, IN 46140, USA.
  • Winkle JR; Elanco Animal Health Research and Development, A Division of Eli Lilly & Company, 2500 Innovation Way, Greenfield, IN 46140, USA.
  • Balko TW; Elanco Animal Health Research and Development, A Division of Eli Lilly & Company, 2500 Innovation Way, Greenfield, IN 46140, USA.
  • Guo S; Shanghai Medicilon, Inc., 585 Chuanda Road, Zhangjiang High-tech Park, Pudong New Area, Shanghai 201200, China.
  • Xue J; Shanghai Medicilon, Inc., 585 Chuanda Road, Zhangjiang High-tech Park, Pudong New Area, Shanghai 201200, China.
  • Cao J; Shanghai ChemPartner, 998 Halei Road, Zhangjiang High-tech Park, Pudong New Area, Shanghai 201203, China.
  • Zou W; BioDuro LLC, Building E, No. 29, Life Science Park Road, Beijing 102206, China.
Bioorg Med Chem Lett ; 25(23): 5589-93, 2015 Dec 01.
Article en En | MEDLINE | ID: mdl-26508546
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 (t1/2=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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos de Boro / Enfermedades de los Perros / Infestaciones Ectoparasitarias / Descubrimiento de Drogas / Isoxazoles Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos de Boro / Enfermedades de los Perros / Infestaciones Ectoparasitarias / Descubrimiento de Drogas / Isoxazoles Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido