B.P. Strunin, L.F. Sattarova, A.F. Ismagilova, I.V. Chudov, N.A. Frolova, S.Y. Garmonov, I.E. Zikova, P.A. Gurevitch

Now in medicine and veterinary science widely used highly active antibacterial preparation belonging to the class 6-fluoro derivatives of 4-hydroxyquinoline-3 carboxylic acids. One of such preparations with a wide spectrum of antibacterial action is 1,4-dihydro-7-piperazil-4-oxo-6-fluoro-1-ethyl-3-quinolinecarboxylic acid (norfloxacin, I). Authors have synthesized an analogue of norfloxacin - 1,4-dihydro-7-(morpholin-4)-4-oxo-6-fluoro-1-ethyl-3-quinolinecarboxylic acid (politril, II). It is recognized that the fragment of morpholine is a part of some medical preparation and, therefore, could expect a manifestation of biological activity. On 578 albino mice and CBA mice and C57B1 weighing 18-20 g and in 184 white rats studied acute toxicity. For the decision of a question on degree of mutagen activity II used a method of the cytogenetic analysis of cages of a marrow. At the same time take into account the chromosomal aberrations of bone marrow cells in mice C57B1. Preparation of 500 mg/kg unitary (entered in doses definition of sharp toxicity), and also in a dose of 5 and 50 mg/kg within 5 days (subchronic activity). In the study took into account single and paired fragments, chromatid and chromosome exchanges. Separately recorded genes gaps. Determination of antibody cells (ASC) in the spleen of the immunized mice was determined using the method of local hemolysis in the liquid phase. For animal immunization as an antigen used sheep erythrocytes, washed three times with saline. Antigen was injected intraperitoneally at an optimal dose 2-108 cells on 20 g of animal weight. Determination of the number of AFC in the spleen of the immunized animals was performed at 5 days after injection of sheep erythrocytes. Slaughtering animals were anesthetized with ether by cervical dislocation. Determination of bacteriostatic activity in vitro was performed by serial dilutions in liquid nutrient medium. Bactericidal activity was studied by the impact of drugs on the test facilities at room temperature and further cultivation of Staphylococcus aureus (strain 209R), Escherichia coli (strain 1749). Bacteriostatic and bactericidal properties were determined visually by the absence of culture growth in the tubes after the daily and incubation for five days at 37 ºC. Based on the study of basic pharmaco-toxicological properties 1,4-dihydro-7-(morpholin-4)-4-oxo-6-fluoro-1-ethyl-3-quinolinecarboxylic acid (politril), found no embryotoxic, mutagenic, sensitizing properties and pronounced anti-inflammatory, and antiulcerogenic immunotropic effect of politril substance, found a pronounced antibacterial activity of politril, which makes it promising for use as an antimicrobial chemotherapeutic agent in veterinary science and medicine.