Biomedical subjects
Publications and source records attributed to F S Mikhaĭlitsyn.
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 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.
Some new bromine (chlorine) derivatives of 8-quinolyloxysalicylanilides were synthesized and tested for trichinellacidal activity. Among them there was the substance N-[3-bromophenyl-4-(5-chloroquinolinoxy)]-3,5-dibromosalicylami de which exhibited its high trichinellocidal activity (in albino mice infected with decapsulated Trichinella spiralis) that was close to that of mebendazole.
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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.
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.
To search for new antihelminthics, the new compound N-[3-chloro-4-[(1-ethyl-2-benzimidazolyl) thio]phenyl]-2-hydroxy-3,5-dibromobenzamide (the agent G-1724) was synthesized and tested by using the models of trichocephaliasis (Trichocephalus muris) and trichinosis (Trichinella spiralis). The tests demonstrated that this agent had an nematocidal effect (71-78%).
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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.
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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.
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