Subject(s)
Anthelmintics/administration & dosage , Chlorides/chemistry , Hymenolepiasis/drug therapy , Hymenolepis nana/drug effects , Sulfides/administration & dosage , Animals , Anthelmintics/chemical synthesis , Disease Models, Animal , Dose-Response Relationship, Drug , Hymenolepiasis/parasitology , Hymenolepis nana/physiology , Mice , Niclosamide/administration & dosage , Parasite Egg Count , Starch/chemistry , Starch/metabolism , Sulfides/chemical synthesis , SuspensionsSubject(s)
Anticestodal Agents/therapeutic use , Benzamides/therapeutic use , Hymenolepiasis/drug therapy , Hymenolepis nana/drug effects , Nitrobenzenes/therapeutic use , Animals , Anticestodal Agents/administration & dosage , Anticestodal Agents/chemistry , Benzamides/chemistry , Benzamides/pharmacology , Disease Models, Animal , Drug Evaluation, Preclinical , Mice , Nitrobenzenes/chemistry , Nitrobenzenes/pharmacologySubject(s)
Anticestodal Agents/therapeutic use , Benzamides/therapeutic use , Bromobenzenes/therapeutic use , Hymenolepiasis/drug therapy , Hymenolepis nana/drug effects , Nitrobenzenes/therapeutic use , Animals , Anticestodal Agents/chemistry , Benzamides/chemistry , Bromobenzenes/chemistry , Drug Evaluation, Preclinical , Nitrobenzenes/chemistryABSTRACT
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.
Subject(s)
Life Cycle Stages/drug effects , Nippostrongylus/growth & development , Ovum/drug effects , Piperidines/chemical synthesis , Piperidines/pharmacology , Tosyl Compounds/chemical synthesis , Tosyl Compounds/pharmacology , Animals , Animals, Outbred Strains , Dose-Response Relationship, Drug , Female , Larva/drug effects , Lethal Dose 50 , Male , Mice , Molecular Structure , Nippostrongylus/drug effects , Piperidines/chemistry , Piperidines/toxicity , Time Factors , Tosyl Compounds/chemistry , Tosyl Compounds/toxicity , Toxicity Tests, AcuteABSTRACT
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.
Subject(s)
Anthelmintics/therapeutic use , Benzamides/therapeutic use , Sulfonamides/therapeutic use , Animals , Drug Evaluation, Preclinical , Halogens/therapeutic use , Helminthiasis/drug therapy , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Anthelmintics/therapeutic use , Benzamides/therapeutic use , Animals , Cricetinae , Drug Evaluation, Preclinical , Echinococcosis/drug therapy , Hymenolepiasis/drug therapy , Mesocricetus , Mice , Opisthorchiasis/drug therapy , Sigmodontinae , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Antimalarials/therapeutic use , Benzamides/therapeutic use , Malaria/drug therapy , Plasmodium berghei , Animals , Antimalarials/toxicity , Benzamides/toxicity , Chloroquine/analogs & derivatives , Chloroquine/therapeutic use , Drug Evaluation, Preclinical , MiceABSTRACT
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.
Subject(s)
Anthelmintics/chemical synthesis , Sulfonamides/chemical synthesis , Animals , Anthelmintics/chemistry , Anthelmintics/toxicity , Chemical Phenomena , Chemistry, Physical , Female , Male , Mice , Sulfonamides/chemistry , Sulfonamides/toxicityABSTRACT
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.