We described here the access to 2-mercapto-4,6-dimethoxy-benzoic acid a key intermediate in the synthesis of the thia-analogue of quercetin. Two syntheses were attempted. The first one using a previously described strategy afforded only very modest yields of the requested compound. The second one which is original is based on the transposition by thermolysis of the appropriately functionalized phenol O-thiocarbamate precursor into the corresponding thiophenol S-thiocarbamate gave fair results which are currently under optimisation.

The etherification of the most commonly used biopolymer i.e. starch in the Williamson reaction with 9-(2-chloroethyl)-carbazole is described. The potato starch was used as the polymeric substrate. The properties of etherate by means of degree of substitution, UV-VIS spectra, IR and the changes in molecular mass are described.

One-pot and facile preparation of novel 2-(4H-4-oxo-benzopyran-3-yl)benzothiazolium salts 3 is described using the fast condensation of 3-formylchromones 1 with 3-benzyl-2-methylbenzothiazolium (or benzoxazolium) bromides 2. Reactions under microwave irradiation, in comparison with classical reactions, proceeded significantly faster and with high yields. Reaction of benzothiazolium salts with secondary and primary amines was also studied. Synthesized chromone derivatives stimulated significantly the growth of the radicle and the hypocotyl at concentrations of 0.1 and 1 ppm, respectively.

A series of new pyrazinamide analogues have been prepared. Report that 5-chloropyrazinamide [1] has different mode of action than pyrazinamide itself [2] promises good chance to reach new structure with high antimycobacterial activity and new action mechanism that is realy needed because of resisance increase [3] to drugs in current use. Dericatives of pyrazine-2,5-dicarbonitrile promise good starting point to further studies (best activity reached yet is 3-(3-chlorophenylamino)pyrazine-2,5-dicarbonitrile, with MIC = 8µmol.l-1 against classical TBC strains and with lower activity against atypical strains. Compared to pyrazinamide with MIC = 4µmol.l-1 against classical strains and no activity against atypical ones).

Unsubstituted, halogenated and/or alkylated pyrazine derivatives connected via -CONH- bridge with substituted anilines were synthesized and tested against Mycobacterium tuberculosis strain H37Rv. Condensation of chlorides of substituted pyrazine-2-carboxylic acids with ring-substituted amines yielded a series of amides of pyrazine-2-carboxylic acid, 6-chloropyrazine-2-carboxylic acid, 5-tert-butylpyrazine-2-carboxylic acid or 5-tert-butyl-6-chloropyrazine-2-carboxylic acid, respectively. The synthetic approach, analytical, spectroscopic, lipophilicity and biological data of twelve newly synthesized compounds are presented. Structure-activity relationships among the chemical structure, the antimycobacterial, antifungal, photosynthesis-inhibiting and antialgal activity of the evaluated compounds are discussed. Pyrazine-2-carboxylic acid (2-trifluormethyphenyl)amide (2) has shown the highest activity against Mycobacterium tuberculosis H37Rv (99% inhibition). The highest antifungal effect against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for 5-tert-butylpyrazine-2-carboxylic acid (3-trifluormethyphenyl)amide (8, MIC = 62.5 µmol mL-1). The highest reduction of chlorophyll content in Chlorella vulgaris was found for 6-chloropyrazine-2-carboxylic acid (3-trifluormethyphenyl)amide (5, IC50 = 12.1 µmol L-1).

A library of new polymerizable functional cross-linking monomers designed for complexation with the oxyanionic moiety of the chemotherapeutic drug methotrexate (MTX). The 1H NMR binding study of a variety of synthetic receptors and the compilation of the obtained results lead to the identification of monomers combining interactive functionality and a cross-linking format, specific binding receptors for dicarboxylate-containing drugs.

The synthesis of hydroxylated butorphanol metabolytes is described.

The molecular recognition features of tolbutamide with four synthetic hosts have been studied by means of NMR titrations, NOESY experiment and Monte Carlo (MC) conformational search. The interaction strength and the most probable structure reveal new insights on the recognition phenomena of this urea derivative in comparison with close related compounds.