Shcherbak O. Antimicrobial activity and biological effects of 4H-pyrido[4', 3': 5,6]pyrano[2,3-d]pyrimidine derivatives

Object of investigation: condensed nitrogen-containing compounds with a pyrimidine cycle, museum and clinical microorganism strains of different taxonomical groups, laboratory animals. Study aim - microbiological substantiation of anti-microbial agents development based on the new derivatives of the nitrogen-containing condensed systems with a pyrimidine fragment. Equipment: microbiological, toxicological, morphological, and statistical. Instruments: torsion scales ВТ-500, microscope "Biolam", electrical thermostat with dry air TS-80, dry-air sterilizer SSS-80, ruler GOST 427-56, microscope Olympus BX-41, PC ASUS K8N-VM. The microbiological screening of the 155 new derivatives of 4Н-pyrido [4',3':5,6]pyrano [2,3-d]pyrymidine was performed for the first time. It was established that certain new compounds possess a profound anti-microbial activity towards the wide range of gram-positive and gram-negative clinically relevant microorganisms, as well as yeast-like, mold fungi and dermatomycetes. It was also established for the first time that the level of antimicrobial activity of the new compounds is dependent on their chemical structure. Also it was show that the speed of resistance development of Candida and Aspergillus fungi to the new synthetic condensed compounds with a pyrimidine fragment is low. According to the experimental results based on the acute toxicity parameters the prospective derivatives can be classified as substances with low toxicity. The influence of the derivatives on the morphological structure of the internal organ tissue of the laboratory animals was studied as well. The obtained results indicate that the search for the new original anti-microbial therapeutic agents based on the new synthetic substanses- 4Н-pyrido [4',3':5,6]pyrano [2,3-d]pyrimidine derivatives can be successful. The level of introduction. 1 patent of Ukraine. A patenting application for an invention № а2011 07115 Ukraine is being filed, the results are being used in the educational process at the departments of organic and toxicological chemistry, microbiology, virology and immunology of the Ukrainian higher education institutions. Field of application: medicine (infectious diseases and complications, mycoses), pharmacy.