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 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.
Subject(s)
Anticestodal Agents/chemical synthesis , Anticestodal Agents/therapeutic use , Hymenolepiasis/drug therapy , Isoquinolines/chemical synthesis , Isoquinolines/therapeutic use , Thiadiazines/chemical synthesis , Thiadiazines/therapeutic use , Animals , Anticestodal Agents/analysis , Anticestodal Agents/toxicity , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Isoquinolines/analysis , Isoquinolines/toxicity , Mice , Praziquantel/analogs & derivatives , Praziquantel/therapeutic use , Praziquantel/toxicity , Spectrophotometry, Infrared/statistics & numerical data , Thiadiazines/analysis , Thiadiazines/toxicityABSTRACT
A procedure has been developed to prepare the anthelminthic Rilanide as a fine-dispersed formulation. The therapeutical dose of the agent in fascioliasis and intestinal nematodiasis is 60 mg/kg (for sheep), if given alone, and 100 mg/kg, if added to feed.
Subject(s)
Anthelmintics/administration & dosage , Anthelmintics/chemical synthesis , Benzene Derivatives/chemical synthesis , Benzene Derivatives/therapeutic use , Fascioliasis/drug therapy , Hydrocarbons, Halogenated/chemical synthesis , Hydrocarbons, Halogenated/therapeutic use , Intestinal Diseases, Parasitic/drug therapy , Nematode Infections/drug therapy , Sheep Diseases/drug therapy , Animals , Anthelmintics/chemistry , Benzene Derivatives/chemistry , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical/veterinary , Fascioliasis/veterinary , Hydrocarbons, Halogenated/chemistry , Intestinal Diseases, Parasitic/veterinary , Nematode Infections/veterinary , SheepABSTRACT
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.
Subject(s)
Anticestodal Agents/chemical synthesis , Antinematodal Agents/chemical synthesis , Benzene Derivatives/chemical synthesis , Intestinal Diseases, Parasitic/veterinary , Monieziasis/drug therapy , Nematode Infections/veterinary , Sheep Diseases/drug therapy , Animals , Anticestodal Agents/therapeutic use , Antinematodal Agents/therapeutic use , Benzene Derivatives/therapeutic use , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Intestinal Diseases, Parasitic/drug therapy , Nematode Infections/drug therapy , Niclosamide/therapeutic use , SheepABSTRACT
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
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).
Subject(s)
Anticestodal Agents/chemical synthesis , Anticestodal Agents/therapeutic use , Echinococcosis/drug therapy , Hymenolepiasis/drug therapy , Quinolines/chemical synthesis , Quinolines/therapeutic use , Animals , Anticestodal Agents/toxicity , Drug Evaluation, Preclinical , Echinococcosis/parasitology , Female , Hymenolepiasis/parasitology , Male , Mebendazole/therapeutic use , Mice , Niclosamide/therapeutic use , Quinolines/toxicity , SigmodontinaeABSTRACT
Manufacturing process for anthelmintic embovin in a micronized form have been developed. Embovin in the micronized form exhibited the highest activity.
Subject(s)
Antinematodal Agents/chemical synthesis , Antinematodal Agents/therapeutic use , Pyrantel Pamoate/chemical synthesis , Pyrantel Pamoate/therapeutic use , Animals , Antinematodal Agents/chemistry , Antinematodal Agents/toxicity , Drug Evaluation, Preclinical , Mice , Nippostrongylus , Pyrantel Pamoate/chemistry , Pyrantel Pamoate/toxicity , Strongylida Infections/drug therapy , Technology, Pharmaceutical/methodsABSTRACT
The authors describe the technology of preparing a new anthelmintic agent triclazan, N-(3,4-dichlorophenyl)-2-[(benzo-2,1,3-thiadiazole-4-sulfonyl)amino]-5- chlorobenzamide, finely dispersed (the particles size 4-8 mu). Triclazan is highly effective not only in hymenolepiasis and trichocephaliasis, as was shown previously, but in fascioliasis, monieziasis and intestinal nematodiasis of sheep as well.
Subject(s)
Anthelmintics/administration & dosage , Anthelmintics/chemical synthesis , Thiadiazoles/administration & dosage , Thiadiazoles/chemical synthesis , Animals , Anthelmintics/chemistry , Cestode Infections/drug therapy , Cestode Infections/veterinary , Drug Evaluation, Preclinical , Nematode Infections/drug therapy , Nematode Infections/veterinary , Particle Size , Sheep , Sheep Diseases/drug therapy , Thiadiazoles/chemistry , Trematode Infections/drug therapy , Trematode Infections/veterinaryABSTRACT
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.
Subject(s)
Antimalarials/chemical synthesis , Heterocyclic Compounds/chemical synthesis , Quinolines/chemical synthesis , Animals , Antimalarials/therapeutic use , Antimalarials/toxicity , Chloroquine/analogs & derivatives , Chloroquine/therapeutic use , Drug Evaluation, Preclinical , Female , Heterocyclic Compounds/therapeutic use , Heterocyclic Compounds/toxicity , Malaria/drug therapy , Male , Mice , Plasmodium berghei , Quinolines/therapeutic use , Quinolines/toxicitySubject(s)
Anthelmintics/chemical synthesis , Benzimidazoles/chemical synthesis , Phthalazines/chemical synthesis , Animals , Anthelmintics/therapeutic use , Anthelmintics/toxicity , Benzimidazoles/therapeutic use , Benzimidazoles/toxicity , Drug Evaluation, Preclinical , Female , Male , Mice , Phthalazines/therapeutic use , Phthalazines/toxicity , Structure-Activity Relationship , Trichinellosis/drug therapyABSTRACT
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.
Subject(s)
Anthelmintics/chemical synthesis , Benzamides/chemical synthesis , Sulfonamides/chemical synthesis , Animals , Anthelmintics/toxicity , Benzamides/toxicity , Female , Lethal Dose 50 , Male , Mice , Structure-Activity Relationship , Sulfonamides/toxicityABSTRACT
The authors describe a method of cultivation and growth peculiarities in a culture of beating cells of the human embryo heart. The influence of homologous anticardiac antibodies and of the ambrosia allergen antiambrosia antibody complex on the contracting cells of the heart of chick and duck embryos was studied in a culture. Pulsation of the cardiac cells was delayed and weakened under the effect of these factors; their vacuolization developed.
