Эффективные методы синтеза 2-гетарил-[1,2,4]триазоло[1,5-c]хиназолин-5(6Н)-онов и их антибактериальная активность

Abstract

INTRODUCTION Microbiological and chemical modifications of natural antibiotics, chemical synthesis of new substances among different classes of organic compounds to obtain new chemotherapeutic agents are key issues of present. It should be noted that quinazoline derivative are interesting in terms of finding new antimicrobial and antifungal agents due to the proven antibacterial activity. AIM To study antimicrobial and antifungal activity among the new derivatives of 2-hetaryl-[1,2,4]triazolo[1,5- с ]quinazolin-5( 6H )-ones. MATERIALS AND METHODS The objects of study are a series of 2-hetaryl-[1,2,4]triazolo[1,5- с ]-quinazolin-5( 6H )-ones (Fig. 1). The minimal inhibitory concentration (MIC) was determined in vitro in the absence of visible growth with minimal drug concentration, minimum bactericidal / fungicidal concentration (MBC / MFC) - the absence of growth on agar after seeding with transparent tubes. Trimethoprim was used as a control of antimicrobial activity of the tested compounds. RESULTS The study of antimicrobial and antifungal activity determined that the synthesized compounds have this activity against Staphylococcus aureus and Escherichia coli . In relation to the Pseudomonas aeruginosa and Candida albicans investigated substances did not show significant bacteriostatic (fungistatic) and bactericidal (fungicidal) activity. CONCLUSIONS A number of efficient methods for the synthesis 2-hetaryl-[1,2,4]triazolo[1,5-с]-quinazolin-5(6H)-ones were developed. The results of studies of the synthesized compounds on the antimicrobial and antifungal activity were shown. It was shown that the highest activity is typical for compounds 2.1 and 2.2, which contain the furan ring.