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English correction fees (250 CHF) will be added in certain cases (1050 CHF per paper for those papers that require extensive additional formatting and/or English corrections.). http://www.mdpi.com/1420-3049/15/12/8567/ A series of sixteen pyrazinamide analogues with the -CONH- linker connecting the pyrazine and benzene rings was synthesized by the condensation of chlorides of substituted pyrazinecarboxylic acids with ring-substituted (chlorine) anilines. The prepared compounds were characterized and evaluated for their antimycobacterial and antifungal activity, and for their ability to inhibit photosynthetic electron transport (PET). 6-Chloro-N-(4-chlorophenyl)pyrazine-2-carboxamide manifested the highest activity against Mycobacterium tuberculosis strain H37Rv (65% inhibition at 6.25 μg/mL). The highest antifungal effect against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for 6-chloro-5-tert-butyl-N-(3,4-dichlorophenyl)pyrazine-2-carboxamide (MIC = 62.5 μmol/L). 6-Chloro-5-tert-butyl-N-(4-chlorophenyl)pyrazine-2-carboxamide showed the highest PET inhibition in spinach chloroplasts (Spinacia oleracea L.) chloroplasts (IC50 = 43.0 μmol/L). For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds as well as their structure-activity relationships are discussed. http://www.mdpi.com/1420-3049/15/12/8567/ Fri, 26 Nov 2010 00:00:00 CET Molecules 2010-11-26 15 12 Article 8567 8581 1420-3049 Synthesis, Antimycobacterial, Antifungal and Photosynthesis-Inhibiting Activity of Chlorinated N-phenylpyrazine-2-carboxamides † 2010-11-26 doi: 10.3390/molecules15128567 Martin Dolezal Jan Zitko Zdenek Osicka Jiri Kunes Marcela Vejsova Vladimir Buchta Jiri Dohnal Josef Jampilek Katarina Kralova http://www.mdpi.com/1420-3049/14/10/4197/ Some [(5Z)-(5-arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)]acetic acids were prepared as potential antifungal compounds. The general synthetic approach to all synthesized compounds is presented. Lipophilicity of all the discussed rhodanine-3-acetic acid derivatives was analyzed using a reversed phase high performance liquid chromatography (RP-HPLC) method. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase using an end-capped non-polar C18 stationary RP column. The RP-HPLC retention parameter log k (the logarithm of the capacity factor k) is compared with log P values calculated in silico. All compounds were evaluated for antifungal effects against selected fungal species. Most compounds exhibited no interesting activity, and only {(5Z)-[4-oxo-5-(pyridin-2- ylmethylidene)-2-thioxo-1,3-thiazolidin-3-yl]}acetic acid strongly inhibited the growth of Candida tropicalis 156, Candida krusei E 28, Candida glabrata 20/I and Trichosporon asahii 1188. http://www.mdpi.com/1420-3049/14/10/4197/ Tue, 20 Oct 2009 00:00:00 CEST Molecules 2009-10-20 14 10 Article 4197 4212 1420-3049 Rhodanineacetic Acid Derivatives as Potential Drugs: Preparation, Hydrophobic Properties and Antifungal Activity of (5-Arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)acetic Acids 2009-10-20 doi: 10.3390/molecules14104197 Jan Dolezel Petra Hirsova Veronika Opletalova Jiri Dohnal Vejsova Marcela Jiri Kunes Josef Jampilek http://www.mdpi.com/1420-3049/14/6/2212/ Eight different functional monomers were used with ethylene glycol dimethacrylate as a cross-linker and molsidomine as a template to obtain molecularly imprinted polymers (MIPs). Non-covalent interactions between molsidomine and each functional monomer in DMSO prior to thermal bulk polymerization were utilized. On the basis of calculated imprinting factors, MIP prepared with N,N’-diallyltartaramide was chosen for further investigations. Examination of interactions in the prepolymerization complex between molsidomine and N,N’-diallyltartaramide was performed using the Job method. The absorbance of isomolar solutions reaching a maximum for the molar ratio of template to monomer equal to 1:4. Scatchard analysis was used for estimation of the dissociation constants and the maximum amounts of binding sites. The polymer based on N,N’-diallyltartaramide has two classes of heterogeneous binding sites characterized by two values of Kd and two Bmax: Kd(1) = 1.17 mM-1 and Bmax(1) = 0.8 μmol/mg for the higher affinity binding sites, and Kd(2) = 200 μM-1 and Bmax(2) = 2.05 μmol/mg for the lower affinity binding sites. Furthermore, effects of pH and organic solvent on binding properties of MIP and NIP were investigated, together with release of molsidomine from both MIP and NIP. http://www.mdpi.com/1420-3049/14/6/2212/ Wed, 17 Jun 2009 00:00:00 CEST Molecules 2009-06-17 14 6 Article 2212 2225 1420-3049 Examination of Imprinting Process with Molsidomine as a Template 2009-06-17 doi: 10.3390/molecules14062212 Piotr Luliński Dorota Maciejewska