[Tanfelam: synthesis, study of ovicidal activity, and acute toxicity]. / Sintez, issledovanie ovitsidnoi aktivnosti i ostroi toksichnosti preparata Tanfelama.

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 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 search for new antiparasitic agents. 18. The synthesis and antitrichinelliasis activity of 1-[(2-acylamino)phenyl]-3,4-dihydroisoquinolines]. / Izyskanie novykh protivoparazitarnykh sredstv. 18. Sintez i protivotrikhinelleznaia aktivnost' nekotorykh 1-[(2-atsilamino)fenil]-3,4-digidroizokhinolinov.

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.

[The technology for manufacturing antiparasitic preparations. 7. Preparation G-1460 and its use for the treatment of monieziasis and intestinal nematodiases]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 7. Preparat G-1460 i ego primenenie dlia lecheniia moniezioza i kishechnykh nematodozov.

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.

[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 technology for manufacturing antiparasitic preparations. 5. The development of a technology for producing the anthelmintic triclonate and the evaluation of its therapeutic efficacy in monieziasis]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 5. Razrabotka tekhnologii polucheniia antigel'mintika triklonata i otsenka ego lechebnoi éffektivnosti pri moniezioze.

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.

[The technology for manufacturing antiparasitic preparations. 4. The development of a technology for producing the anthelmintic bromoksan in finely dispersed form and the evaluation of its antifascioliasis activity]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 4. Razrabotka tekhnologii polucheniia antigel'mintika bromoksana v melkodispersnoi forme i otsenka ego protivofastsioleznoi aktivnosti.

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.

[The synthesis and study of the acute toxicity and anthelmintic activity of new 2-methylthiobenzimidazoles]. / Sintez, izuchenie ostroi toksichnosti i protivogel'mintnoi aktivnosti novykh 2-metiltiobenzimidazolov.

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.

[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 technology for manufacturing antiparasitic preparations. 3. The development of a technology for producing the anthelmintic embovin (pyrantel embonate) in finely dispersed form and the evaluation of its anthelmintic properties]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 3. Razrabotka tekhnologii polucheniia antigel'mintika émbovina (pirantelia émbonata) v melkodispersnoi forme i otsenka ego protivogel'mintnykh svoistv.

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

[The synthesis and study of the acute toxicity and anthelmintic activity of salicylanilides containing a quinoline residue]. / Sintez, izuchenie ostroi toksichnosti i protivogel'mintnoi aktivnosti salitsilanilinov, soderzhashchikh ostatok khinolina.

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.

[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. 10. The synthesis, toxicological and antimalarial properties of nitrogen-containing heterocycles with a 4-(4-alkylpiperazinyl-1) phenylamine substituent (the preparation quinoprazine)]. / Izyskanie novykh protivoparazitarnykh sredstv. 10. Sintez, toksikologicheskkie i protivomaliariinye svoistva nekotorykh azotsoderzhashchikh geterotsiklov s 4-(4-alkilpiperazinil-1)fenilaminnym zamestitelem (preparat khinoprazin).

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 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.