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The papers describes the synthesis of N-(2-piperidinoethyl)-N-tosyl-n-anisidine (Tanfelam) which showed a 100% ovicidal activity when tested by the Harada and Mori methods (in vitro inhibited N.brasiliensis hatching and development test). Tanfelam has been transferred for in-depth tests.

The paper describes a procedure for manufacturing the new anthelminthic Tizanox. It shows it necessary to administer a larger dose of the drug than that of azinox (praziquantel) to treat experimental hymenolepiasis. However, the lower toxicity of Tizanox enhances its chemotherapeutical index.

New 1-[(2-acylamino)phenyl]-3, 4-dihydroisoquinolines were synthesized and tested for their acute toxicity and antitrichinosis activity. The above compounds were found to show their low toxicity and two compounds (G-1615 and G-1616) displayed a high antitrichinosis effect.

A procedure was developed for the synthesis of the anthelminthic G-1460. The therapeutical doses (20 and 25 mg/kg) of the agent were defined for the treatment of monieziasis and gastrointestinal nematodes on an individual basis.

A procedure has been developed to manufacture the anthelminthic Triclonate. The agent was tested for the treatment of sheep's natural monieziasis infection and it was found to have a high activity.

A manufacturing procedure has been developed to prepare the anthelmintic bromoxane as a finely divided dosage form. The maximum toxic dose of the drug was 1 g per kg mice body weight. Its therapeutic dose in sheep fascioliasis was 20 mg/kg.

Several derivatives of 2-methylthiobenzimidazoles were synthesized and assayed for anthelmintic activity. Following these studies, 2-methylthio-5-(1-chloronaphthyloxy-2)-6-chlorobenzimidazole (G-1557) has been selected as a tichinellacide for detailed investigations.

Manufacturing process for anthelmintic embovin in a micronized form have been developed. Embovin in the micronized form exhibited the highest activity.

Salicylanilides containing quinoline moiety were synthesized and examined for acute toxicity and antinematodal activity. All the compounds were shown to possess a low toxicity. In the trials on a nematodal model (Aspiculuris tetraptera, white mice), 2 compounds--G-1570 and G-1575--were shown to be highly effective.

Synthesis is described and acute toxicity and antimalaria action is studied in new derivatives of quinoline and benzo(g)quinoline containing a 4-(4-alkylpiperazinyl-1)phenylamine substitute. Only the derivatives of benzo(g)quinoline were found to have a high antimalaria effect and to have advantages over the standard agent chloroquine on their tolerance and protective action. One of the compounds, 4-[4-(4-ethylpiperazinyl-1)phenylamino] benzo(g)quinoline, named QUINOPRAZINE, showed some action against Plasmodium berghei chloroquine--resistant infection (isolate LN-K65). This agent was elected for further tests.

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.

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.

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.

Antimalarial activity of 10 N-(haloidnaphthyloxy)-2-hydroxy-3,5-dihaloidbenzamide compounds earlier synthesized as potential anthelmintics has been studied. It has been shown that antimalarial activity is typical only of amides of 2-hydroxy-3,5-diiodinebenzoic acid.

Sulfamidobenzamides containing benzo-2,1,3-thiadiazole ring in the sulfamide group were synthesized and examined for acute toxicity. All the compounds were shown to have low toxicity (when administered orally in a dose of 4 g/kg to mice), the above fact makes possible the search for agents with anthelminthic activity.

Novel derivatives of sulfamidobenzamides have been synthesized and tested for acute toxicity. All the compounds were shown to possess a low toxicity. It was suggested that the investigated sulfamidobenzamides might be a promising group among which to search for agents having anthelminthic activity.

The paper presents the results of toxicological study of 44 compounds of the benzamide series synthesized during search for new anthelminthic agents. The dependence of the toxic effect of the benzamides synthesized on their structure is analysed. The experiments were carried out on white mice given the compounds under study once orally. The maximum tolerated doses of the compounds are presented. It has been found that 34 out of 44 compounds have a low toxicity and are worth of further anthelminthic screening.