[The technology for manufacturing antiparasitic preparations. 6. The development of a technology for producing the anthelmintic Azinox (praziquantel) and the evaluation of its toxic and anthelmintic properties]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 6. Razrabotka tekhnologii polucheniia antigel'mintika Azinoksa (prazikvantelia) i otsenka ego toksicheskikh i protivogel'mintnykh svoistv.

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.

[The efficacy of entomopathogenic bacilli against ancylostomide larvae--Nippostrongylus braziliensis Travassons, 1914]. / Effektivnost' éntomopatogennykh batsill protiv lichinok ankilostomid--Nippostronylus braziliensis Travassons, 1914.

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.

[The structure and anthelmintic action of tricyclic analogs of praziquantel and 4-acylpiperazinones-2]. / Stroenie i antigel'mintnaia aktivnost' tritsiklicheskikh analogov prazikvantelia i 4-atsilpiperazinonov-2.

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 search for new antiparasitic agents. 9. The anthelmintic activity of halogen-containing sulfonamidobenzamides]. / Izyskanie novykh protivoparazitarnykh sredstv. 9. Protivogel'mintnaia aktivnost' galoidsoderzhashchikh sul'fonamidobenzamidov.

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.

[The search for new antiparasitic agents. 8. The synthesis and study of the acute toxicity, anti-alveolar hydatid and antihymenolepiasis activity of 1-alkyl-4[4-(heterylamino)phenyl]piperazines]. / Izyskanie novykh protivoparazitarnykh sredstv. 8. Sintez i issledovanie ostroi toksichnosti, protivoal'veokokkoznoi i protivogimenolepidoznoi aktivnosti nekotorykh 1-alkil-4[4-(geterilamino)fenil]piperazinov.

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.

[The search for new antiparasitic agents. 7. A study of the relationship between the structure and the anthelmintic activity of new halogen-containing benzamides]. / Izyskanie novykh protivoparazitarnykh sredstv. 8. Izuchenie sviazi mezhdu stroeniem i protivogel'mintnoi aktivnost'iu novykh galoidsoderzhashchikh benzamidov.

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.