[Activity of the anthelmintic agent trichlorophen on the models of human helminthiasis]. / Aktivnost' otechestvennogo antigel'mintika trikhlofena na modeliakh gel'mintozov cheloveka.

Trials of trichlorophen have shown its high efficacy on models of cestode infections: hymenolepiasis (at the adult and cysticercoid stages of development on three types of animals: outbred albino mice, albino rats and golden hamsters), preimaginal echinococciasis alveolaris, larval alveolar echinococciasis (at the early stage of development of the parasite in experiments on cotton rats). The high nematodical activity of trichlorophen was first found on models of trichocephaliasis in DBA/2y mice, nippostrongyloidiasis (in in vitro experiments), and aspiculuriasis in outbred mice. The agent proved to be ineffective at the tissue developmental stage of Hymenolepsis nana (H. nana), the dwarf tapeworm, in albino mice, during experimental opisthorchiasis in golden hamsters. It showed a low efficacy in treating trichinosis in outbred albino mice. Unlike carbamatebenzimidazoles, trichlorophen was inactive at the tissue stage of H. nana; it exerted no effects on the eggs of a dwarf tapeworm in trichinosis. Trichlorophen was also inactive in treating experimental opisthorchiasis in golden hamsters.

[Developing of new anthelmintics. Evaluation of fluzamide on the new experimental models of intestinal cestode infections]. / Razrabotka novykh otechestvennykh antigel'mintikov. Otsenka terapevtitseskoi aktivnosti fluzamida na novykh éksperimental'nykh modeliakh kishechnykh tsestodozov.

The efficacy of the original drug fluzamide (a N,S-containing heterocycle derivative) was evaluated by primary screening on a modified model of monoinvasion with the luminal form of Echinococcus multilocularis and on an original model of intestinal mixed invasion of E. multilocularis and Hymenolepsis nana at the immature and mature stages of the parasites in golden hamsters when an experimental host was immunosuppressed with hydrocortisone. The efficacy of fluzamide in an oral dose of 0.3 g/kg against young E. multilocularis and H. nana (the duration of their invasion was 7 days) was 99.8-100%; that against adult cestodes of both species (their maximum age was 28 days) was 100%. The original method of simulation of intestinal cestodiases in laboratory rodents, which is based on the artificial transplantation of cestodes at the prepatent stage of development from the intestine of infected donors to the intestine of healthy recipients through the latter' stomach during drug immunosuppression, showed its high reliability. There is evidence that transplanted immature strobilar cestodes can survive in the stomach, get acclimated, and continue to develop in the recipients' small bowel up to the stage of formation of infective eggs.

[The technology for manufacturing antiparasitic preparations. 9. The new preparation tizanox and an evaluation of its anti-Hymenolepis activity]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 9. Novyi preparat tizanoks i otsenka ego protivogimenolepidoznoi aktivnosti.

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.

[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 search for new antiparasitic agents. 17. The synthesis and study of the anti-echinococcal activity of the new preparation G-1697]. / Izyskanie novykh protivoparazitarnykh sredstv. 17. Sintez i izuchenie protivoékhinokokkovoi aktivnosti novogo preparata G-1697.

The paper describes the synthesis of the new agent G-1697 which is 4-[(benzo-2,1,3-thiadiazolyl-4)amino]-5, 6,7,8-tetrahydrobenzothieno [2,3-d] pyrimidine and the results of testing its acute toxicity and antiparasitic activity on a model of Echinococcus multilocularis invasion at the larval stage in cotton rats. The maximum nonlethal dose of G-1697 was 4.0 g/kg for outbred mice of both sexes whose weight was 14-16 g. Adult cotton rats (males) received the agent with their feed in increasing daily doses for 3 weeks continuously on days 8 to 28 after infection. The daily dose of its active ingredient varied from 0.03 to 0.35 g/kg and averaged 0.12 g/kg (the mean total dose per session was 2.47 g/kg). The baseline weight of parasitic larvocysts (PL) per animal averaged 0.28 g at the baseline. In the treated and control rats sacrificed 34 days following infection, the mean mass of PL per animal was 0.95 and 7.51 g, respectively. In the cotton rats treated with G-1697, the suppressed growth index calculated by three parameters (moderate, maximum, and minimum mass of PL in the animals of the comparable groups after treatment with regard to the similar baseline variables) was 90.8, 91.0 and 92.7, respectively, versus the controls. Among all PL found in each animal, its death was approximately 70-90% in the treated rats.

[The search for new antiparasitic agents. 12. The synthesis and study of the anti-Echinococcus and anti-Hymenolepis activity of 6-[4-(4-alkylpiperazinyl-1)-phenylamino]-1,2,5-thiadazolo[3 ,4-h] quinolines]. / Izyskanie novykh protivoparazitarnykh sredstv. 12. Sintez i izuchenie protivoékhinokokkoznoi i protivogimenolepidoznoi aktivnosti 6-[4-(4-alkilpiperazinil-1)-fenilamino]-1,2,5-tiadiazolo[3,4-h] khinolinov.

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).

[The search for new antiparasitic agents. 11. The acute toxicity and anticestodal activity of the new anthelmintic Tizanox compared with Azinox]. / Poisk novykh protivoparazitarnykh sredstv. 11. Ostraia toksichnost' i protivotsestodnaia aktivnost' novogo antigel'mintika tizanoksa v sravnenii s azinoksom.

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.

[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.