Σχεδιασμός, σύνθεση και μελέτη βιολογικής δράσης θειαζολικών παραγώγων

Abstract

This thesis presents and discusses the design, synthesis and evaluation ofbiological activity of twenty-two (22) novel thiazole derivatives, twelve (12) of whichare chalcones, two (2) aminopyrimidines and eight (8), N-phenylpyrazolines.Prediction of biological activity spectra for all compounds was performed bythe program PASS.The aim was to design compounds that would combine antimicrobial and antiinflammatoryactivity, taking into account the wide spectrum of biological activitiesof thiazole derivatives, as well as, the interesting pharmacological properties ofchalcones, aminopyrimidines and N-phenylpyrazolines.The final compounds were identified by elemental analysis and spectroscopicmethods.Σheoritical calculations of several physicochemical parameters, includinglipophilicity, were performed for all final compounds.The evaluation of antimicrobial activity of the compounds against selected Gram(+) and Gram (-) bacteria and fungi was carried out in vitro using microdilution method.For a number of selected compounds, DNA gyrase inhibition assay was alsoperformed, in order to explain the possible mechanism of their antibacterial activity.The in vivo evaluation of anti-inflammatory activity of compounds was carriedout by use of carrageenin induced mouse paw edema model, while selected compoundswere also tested in vitro for their ability to inhibit cycloxygenase (COX 1 and 2).