[The Soviet antimalarial preparation dabequine studied for the presence of mutagenic activity].
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Biomedical subjects
Publications and source records attributed to M N Lebedeva.
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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.
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 study covers the study of three antinematodal agents: the original national drug medamine with albendazole and embovin (pyrathel pamoate), which have been reproduced at the E. I. Martsinovskiĭ Institute of Medical Parasitology and Tropical Medicine, with murine Syphacia obvelata and Aspiculuris tetraptera infection models. The quantitative parameters of the anthelmintic action of medamine, albendazole and embivin were comparatively defined for the first time.
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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).
Manufacturing process for anthelmintic embovin in a micronized form have been developed. Embovin in the micronized form exhibited the highest activity.
Pharmacokinetic studies of a new anthelminthic tegalid, made in this country, were carried out. The drug concentrations in biologic material were measured by high-pressure liquid chromatography. The drug was found to circulate for a rather long time in the blood, virtually not accumulating in any of the examined organs, except the liver. Tegalid pharmacokinetics can be fairly well approximated by a unicompartmental model with due consideration for its absorption.
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.
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