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1.
Vet Dermatol ; 25(3): 195-e49, 2014 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-24797425

RESUMEN

BACKGROUND: Canine flea-allergy dermatitis (FAD), a hypersensitivity response to antigenic material in the saliva of feeding fleas, occurs worldwide and remains a common presentation in companion animal veterinary practice despite widespread availability of effective systemic and topical flea-control products. HYPOTHESIS/OBJECTIVES: To evaluate the clinical response in dogs with FAD treated topically with indoxacarb, a novel oxadiazine insecticide. ANIMALS: Twenty-five client-owned dogs in Queensland, Australia diagnosed with pre-existing FAD on the basis of clinical signs, flea-antigen intradermal and serological tests. METHODS: An open-label, noncontrolled study, in which all dogs were treated with topical indoxacarb at 4 week intervals, three times over 12 weeks. RESULTS: Twenty-four dogs completed the study. Complete resolution of clinical signs of FAD was observed in 21 cases (87.5%), with nearly complete resolution or marked improvement in the remaining three cases. Mean clinical scores (Canine Atopic Dermatitis Extent and Severity Index-03) were reduced by 93.3% at week 12. Mean owner-assessed pruritus scores were reduced by 88% by week 12. Mean flea counts reduced by 98.7 and 100% in weeks 8 and 12, respectively. CONCLUSIONS AND CLINICAL IMPORTANCE: Topical indoxacarb treatment applied every 4 weeks for 12 weeks, without concomitant antipruritic or ectoparasiticide therapy, completely alleviated flea infestations in all dogs and associated clinical signs of FAD in a high proportion of this population of dogs in a challenging flea-infestation environment.


Asunto(s)
Dermatitis Alérgica por Contacto/veterinaria , Enfermedades de los Perros/parasitología , Infestaciones por Pulgas/veterinaria , Oxazinas/farmacología , Siphonaptera/efectos de los fármacos , Administración Tópica , Animales , Dermatitis Alérgica por Contacto/tratamiento farmacológico , Enfermedades de los Perros/tratamiento farmacológico , Perros , Femenino , Infestaciones por Pulgas/tratamiento farmacológico , Insecticidas/administración & dosificación , Insecticidas/farmacología , Masculino , Oxazinas/administración & dosificación , Siphonaptera/inmunología
2.
Bioorg Med Chem Lett ; 21(14): 4160-3, 2011 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-21684739

RESUMEN

A series of 2-phenylimidazo[1,2-b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD(99) values of 30nM, which is comparable to that of the benchmark commercial nematocide, Ivermectin.


Asunto(s)
Antinematodos/química , Haemonchus/efectos de los fármacos , Piridazinas/química , Animales , Antinematodos/síntesis química , Antinematodos/farmacología , Haemonchus/crecimiento & desarrollo , Ivermectina/química , Ivermectina/farmacología , Larva/efectos de los fármacos , Piridazinas/síntesis química , Piridazinas/farmacología , Relación Estructura-Actividad
3.
Bioorg Med Chem Lett ; 20(2): 649-52, 2010 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-19962303

RESUMEN

A series of hydrazonotrifluorosulfonanilide derivatives were synthesized and evaluated for in vitro activity against the ectoparasites Ctenocephalides felis and Rhipicephalus sanguineus. Some compounds with excellent activity against tick were identified.


Asunto(s)
Antiparasitarios/química , Hidrazonas/química , Sulfonamidas/química , Animales , Antiparasitarios/síntesis química , Antiparasitarios/farmacología , Gatos , Perros , Descubrimiento de Drogas , Hidrazonas/síntesis química , Hidrazonas/farmacología , Rhipicephalus sanguineus/efectos de los fármacos , Relación Estructura-Actividad , Sulfonamidas/síntesis química , Sulfonamidas/farmacología
4.
Bioorg Med Chem Lett ; 18(1): 252-5, 2008 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-18006308

RESUMEN

A series of novel 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilide derivatives have shown significant in vitro parasiticidal activity against the ectoparasites Ctenocephalides felis and Rhipicephalus sanguineus. A number of these compounds also displayed significant in vitro endoparasite activity against the nematode Haemonchus contortus.


Asunto(s)
Antiparasitarios/química , Antiparasitarios/farmacología , Rhipicephalus sanguineus/efectos de los fármacos , Siphonaptera/efectos de los fármacos , Sulfonamidas/química , Sulfonamidas/farmacología , Animales , Haemonchus/efectos de los fármacos , Relación Estructura-Actividad
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