The aim of the Thesis is to develop new potent inhibitors of HK TCs based on fragmentbased lead discovery approach and virtual screening hits. Concomitantly new methods of synthesis of the most potent heterocyclic motifs may be explored. The following tasks were set: 1) to synthesize putative HK TCs inhibitors designed by project partners – derivatives of pyrazole, quinazoline and indazole heterocyclic motifs – and analyze their structureactivity relationship (SAR) using the data provided by collaboration institutions; 2) to explore novel milder ways of assembling of the most perspective 2-aminoquinazoline and indazole scaffolds, starting from readily available 2-formylphenylboronic acids; 3) to synthesize 3,4-diphenylpyrazole derivatives with proved antimicrobial activity, possibly connected with inhibition of HK TCs, and analyze their SAR regarding inhibition of growth of S. Aureus Newman.