EXPERIMENTAL STUDY OF SPECIFIC ACTIVITY OF 1,3-DIAZINON-4 COMPOUND PYaTdl DERIVATIVE IN VIVO

Aim. Study anti-leprosy activity of a 1.3-diazinon-4 compound derivative under the laboratory code PYaTd 1 on the model of intra-plantar infection of mice and evaluate the character of its antibacterial effect. Materials and methods. Study of specific activity was carried out in vivo on the experimental model of leprosy, proposed by Shepard C.C., that assumes execution of intra-plantar infection of mice with a suspension of mycobacteria, produced from lepromas or autopsy tissue of a non-treated leprosy infected, or from tissues of experimental mice, previously infected with Mycobacterium leprae from non-treated patients. The study was carried out on 120 C BA line mice infected with M. leprae (VIII passage) from patient M. Dapsone and PYaTdl compound were administered to animals next day after the infection with forage at a dose of 25 mg/kg for 4.5, 6, 9 and 11 months. The mice were split into 3 groups: control (infected without treatment), comparison (infected, receiving dapsone), experimental (infected, receiving PYaTd 1). After the control term the mice were euthanized under chloroform anesthesia. Suspensions for quantification of mycobacteria were prepared from paw pads. Smears were stained by Ziehl-Nilsson. Results. After 4.5 months the intensity of infect reproduction under the effect of dapsone and PYaTd 1 was reduced compared with control by 18 - 25 times. After a 6-month course - by 50 - 75% and after 9 months - by 85 - 90%. After 11 months in mice that had received PYaTd 1, an intensive suppression of microorganism reproduction was observed: the yield in paws was 70 times lower than in control. In the group that had received dapsone, a reduction of the number of mycobacteria by 20 - 25 times was detected, it was significantly less effective than under the conditions of PYaTd 1 administration. Conclusion. A novel 1.3-diazinon-4 derivative under the code PYaTdl can actively supress reproduction of M. leprae, that gives evidence regarding its specific anti-mycobacterial activity and determines perspectives of its further studies.

3-диазинона-4 ПЯТ61, anti-leprosy activity, 1.3-diazinon-4 derivative PYaTdl, Shepard C.C. model, M. leprae