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The Petasis reaction of 6-alkoxy adducts of 1-alkyl-2,3-dicyano-5-arylpyrazinium salts with aromatic boronic acids, such as 2-thienylboronic, 2-furanylboronic and 3-thienylboronic acids, or their benzo analogs in dichloromethane proceeds smoothly at room temperature with the formation of the corresponding 5-aryl-6-hetaryl substituted 1,6-dihydropyrazine derivatives. All dihydropyrazines were separated as pure enantiomers by chiral HPLC, and their absolute configurations for each pair of enantiomers have been determined by X-ray analysis. Individual enantiomers were screened in vitro for their antimycobacterial activities against Mycobacterium tuberculosis H 37 Rv, avium, terrae and extensively drug-resistant and multi-drug-resistant strains isolated from tuberculosis patients in Ural region (Russia). It has been shown that several compounds exhibit a good level of antituberculosis activity compared to the reference drugs.

Background: The problem of increasing antibiotic resistance, decrease in the quality of treatment and its inefficiency, the prolongation of terms of hospitalization, development of nosocomial infections, and increasing treatment costs leads to significant social and financial losses. Based on international recommendations and consideration of the microbial landscape the local strategy for the use of antibacterial drugs was developed and implemented. Methods: In this study, an analysis of the effectiveness of the rational use of antibiotics comparing results of 2014 and 2015 was conducted: Selection of the most significant nosocomial pathogens and determination of their antibiotic susceptibility (in percentages) ABC / VEN-analysis of antimicrobial agents Calculation of ATC / DDD usage of antimicrobials Results: of 2015 compared to 2014: Despite the growth of antibiotic resistance strains of Acinetobacter spp, improvement in antibiotic susceptibility is noticable (depending on the drug) Staphilococcus aureus from 2.5% to 38.8%; Pseudomonas aeruginosa from 1.1% to 13.2%; Klebsiella pneumonia from 5% to 40.3%; E coli 5,5-32,2%.The decrease in the cost of antibiotics by 3.8%. The decrease in ATC / DDD consumption (for 22 antibiotics), except for piperacillin tazobactam with the DDD 0.47 to 0.66; meropenem from 1.69 to 2.23; cefoperazone / sulbactam from 0.39 to 0.79 and gentamicin from 0.13 to 48.99. Conclusions: Ongoing efforts to rationalize the use of antimicrobials and the containment of antimicrobial resistance in a multidisciplinary hospital should be comprehensive, in coordination of representatives of different specializations, which in the future will increase efficiency of treatment and reduce the hospitalization time of the patient.Even minor positive indicators give hope that activities were carried out in the right direction.