Subject(s)
Anthelmintics/therapeutic use , Benzamides/therapeutic use , Hymenolepiasis/drug therapy , Hymenolepis nana , Thiadiazoles/therapeutic use , Administration, Oral , Animals , Anthelmintics/toxicity , Benzamides/chemistry , Benzamides/toxicity , Drug Evaluation, Preclinical , Mice , Molecular Structure , Structure-Activity Relationship , Thiadiazoles/chemistry , Thiadiazoles/toxicityABSTRACT
The paper outlines a procedure for manufacturing the anthelminthic Azinox (biltricide) using the new interfacial transfer catalyst benzyl-di-propyl (beta-hydroxyethyl)ammonium chloride. Azinox has been shown to be identical to biltricide (praziquantel) in its properties. Azinox tests on models of Opisthorchis felineus in golden hamsters and of Hymenolepis nana in albino outbred mice have indicated that the agent is not inferior to biltricide in its antitrematodal and anticestodal activities. Azinox displayed a high activity at the preimaginal stages of O. felineus and H. nana and at the larval stage of H.nana.
Subject(s)
Anticestodal Agents/chemical synthesis , Antiplatyhelmintic Agents/chemical synthesis , Praziquantel/analogs & derivatives , Animals , Anticestodal Agents/therapeutic use , Anticestodal Agents/toxicity , Antiplatyhelmintic Agents/therapeutic use , Antiplatyhelmintic Agents/toxicity , Cricetinae , Drug Evaluation, Preclinical , Female , Hymenolepiasis/drug therapy , Hymenolepiasis/parasitology , Lethal Dose 50 , Male , Mesocricetus , Mice , Opisthorchiasis/drug therapy , Opisthorchiasis/parasitology , Praziquantel/chemical synthesis , Praziquantel/therapeutic use , Praziquantel/toxicityABSTRACT
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.
Subject(s)
Antinematodal Agents/toxicity , Bacillus , Insecticides/toxicity , Nippostrongylus/drug effects , Animals , Bacillus thuringiensis , Bacterial Toxins/toxicity , Dose-Response Relationship, Drug , Larva/drug effects , Spores, Bacterial , TemperatureABSTRACT
The toxicity and anthelminthic activity of the earlier synthetized tricyclic analogues of praziquantel and 4-acylpiperazinones-2 have been studied. Tricyclic compounds have shown the acute toxicity similar to that of praziquantel and neurotoxic effect typical of praziquantel. 4-acylpiperazinones-2 toxicity correlated with their anthelminthic effect. The determination of anthelminthic activity of the above compounds in opisthorchiasis and hymenolepiasis has shown that they are less effective than praziquantel or have no anthelminthic activity. A biological activity-structure relationship has been traced in the compounds under study.
Subject(s)
Anthelmintics/toxicity , Piperazines/toxicity , Praziquantel/analogs & derivatives , Animals , Anthelmintics/therapeutic use , Cricetinae , Drug Evaluation, Preclinical , Female , Hymenolepiasis/drug therapy , Lethal Dose 50 , Male , Mesocricetus , Mice , Opisthorchiasis/drug therapy , Piperazines/therapeutic use , Praziquantel/therapeutic use , Praziquantel/toxicity , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Anthelmintics/therapeutic use , Benzamides/therapeutic use , Sulfonamides/therapeutic use , Animals , Drug Evaluation, Preclinical , Halogens/therapeutic use , Helminthiasis/drug therapy , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Anticestodal Agents/chemical synthesis , Echinococcosis/drug therapy , Hymenolepiasis/drug therapy , Piperazines/chemical synthesis , Animals , Anticestodal Agents/therapeutic use , Anticestodal Agents/toxicity , Drug Evaluation, Preclinical , Female , Male , Mice , Piperazines/therapeutic use , Piperazines/toxicity , SigmodontinaeABSTRACT
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.
