| Summary: | TB remains a major cause of population mortality in the world. Research of new substances with antimycobacterial activity is emphasized also because of increasing occurrence of resistance in case of monotherapy as well as combination therapy with AT of first and second line. Current trends in the development rest in the connection of two molecules into one - the so-called double active compound - by means of various linkers. In the process of synthesis of 2-isonicotinoyl-N-substituted phenylhydra- zinecarboxamides, a carbonyl bridge was used. The synthesis of these substances was realized by two methods. In the first one, the reaction was based on substituted isocyanate; in the second one, preparation of isocyanate in situ from a substituted aniline using triphosgene was applied. All substances were tested for in vitro antimycobacterial activity. The substance 2-isonicotinoyl-N-(2,4,6-trichlorophenyl)hy- drazinecarboxamide exhibited the highest activity against Mycobacterium tuberculosis 331/88 with MIC value (4 μmol/L). The compounds were also tested for other strains of mycobacteria - Mycobacterium avium 330/88, Mycobacterium kansasii 235/80 and Mycobacterium kansasii 6509/96. Synthesis of N-substituted phenyl-5-(pyridine-4-yl)- 1,3,4-oxa-diazol-2-amines was based on the selected and prepared...
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