Assuntos
Anti-Helmínticos/uso terapêutico , Benzamidas/uso terapêutico , Himenolepíase/tratamento farmacológico , Hymenolepis nana , Tiadiazóis/uso terapêutico , Administração Oral , Animais , Anti-Helmínticos/toxicidade , Benzamidas/química , Benzamidas/toxicidade , Avaliação Pré-Clínica de Medicamentos , Camundongos , Estrutura Molecular , Relação Estrutura-Atividade , Tiadiazóis/química , Tiadiazóis/toxicidadeRESUMO
The paper describes the synthesis of 6-[4-alkylpiperazinyl-1)phenylamino]-1,2,5-thiadiazolo[3,4-h ]quinolines where methyl (Drug G-1574) and ethyl (Drug G-1569) are alkyls. The two agents are as effective as mebendazole against the larval stage of Echinococcus multilocularis infection. Drug G-1574 has been demonstrated to ensure 100% recovery of spontaneously Hymenolepis nana-infected albino mice given doses 2.5-5 times lower than the effective dose of phenasal (niclosamide).
Assuntos
Anticestoides/síntese química , Anticestoides/uso terapêutico , Equinococose/tratamento farmacológico , Himenolepíase/tratamento farmacológico , Quinolinas/síntese química , Quinolinas/uso terapêutico , Animais , Anticestoides/toxicidade , Avaliação Pré-Clínica de Medicamentos , Equinococose/parasitologia , Feminino , Himenolepíase/parasitologia , Masculino , Mebendazol/uso terapêutico , Camundongos , Niclosamida/uso terapêutico , Quinolinas/toxicidade , SigmodontinaeRESUMO
Effects of seven bioinsecticides, containing Bacillus thuringiensis and B. sphaericus toxins, against N. braziliensis larvae were studied in vitro. Bitoxibacillin, astur-3, astur-4, gomelin, lepidocide, dendrobacillin, thuringin and sphaerix were found highly effective larvicides. Protein endotoxin was the principal component responsible for the larvicidal effect, the spores were of no importance.
Assuntos
Antinematódeos/toxicidade , Bacillus , Inseticidas/toxicidade , Nippostrongylus/efeitos dos fármacos , Animais , Bacillus thuringiensis , Toxinas Bacterianas/toxicidade , Relação Dose-Resposta a Droga , Larva/efeitos dos fármacos , Esporos Bacterianos , TemperaturaRESUMO
A synthesis is described and the results of toxicological trial of the potential anthelmintic agent G-1587 are presented. The agent is 2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-2H-[1, 2,5] thiadiazino [3,2-a] isoquinoline-4,4-dioxide. The agent was shown to have a low toxicity, the maximal sublethal dose for mice being 4.0 g/kg when given per os.
Assuntos
Anticestoides/toxicidade , Isoquinolinas/toxicidade , Praziquantel/análogos & derivados , Tiadiazinas/toxicidade , Animais , Anticestoides/uso terapêutico , Cricetinae , Avaliação Pré-Clínica de Medicamentos , Equinococose/tratamento farmacológico , Feminino , Himenolepíase/tratamento farmacológico , Isoquinolinas/uso terapêutico , Dose Letal Mediana , Masculino , Mesocricetus , Camundongos , Praziquantel/uso terapêutico , Praziquantel/toxicidade , Tiadiazinas/uso terapêuticoRESUMO
The results of preclinical trials of 28 new compounds of haloid-containing sulfamidobenzamides with low toxicity are presented. The trials on a hymenolepiasis model showed that effectiveness of N-(2,5-dichlorophenyl)-2/(3-nitro-4-chlorophenyl) sulfonylamino/-5-bromobenzamide was similar to that of the well-known drug niclosamide. In the trials on an opisthorchiasis model, 2 compounds were shown to be highly effective, and on a trichocephaliasis model 5 compounds showed a high activity.
Assuntos
Anti-Helmínticos/uso terapêutico , Benzamidas/uso terapêutico , Sulfonamidas/uso terapêutico , Animais , Avaliação Pré-Clínica de Medicamentos , Halogênios/uso terapêutico , Helmintíase/tratamento farmacológico , Relação Estrutura-AtividadeRESUMO
The synthesis and the acute toxicity and anticestodal activity of l-alkyl-4-[-(heterylamino)phenyl]-piperazines are presented. These compounds were found to be able to suppress the growth of larvocysts of Echinococcus multilocularis in cotton rats when injected intraperitoneally in a single dose of 0.25 g/kg, close to capacity of mebendazole. The tested compounds were also highly effective against the adult stage of Hymenolepis nana. Experimentally infected mice given an oral single dose of 0.2-0.5 g/kg of the drug were radically cured.
Assuntos
Anticestoides/síntese química , Equinococose/tratamento farmacológico , Himenolepíase/tratamento farmacológico , Piperazinas/síntese química , Animais , Anticestoides/uso terapêutico , Anticestoides/toxicidade , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Camundongos , Piperazinas/uso terapêutico , Piperazinas/toxicidade , SigmodontinaeRESUMO
Anthelminthic properties of new series of haloid-containing benzamides have been studied. The anthelminthic activity-structure relationships of the compounds under study has been examined. A number of highly active compounds promising for further investigations have been identified.