Yeni bazı 2-benzil-5 sübstitüe benzoksazol türevlerinin sentezi, yapılarının aydınlatılması, kemoterapötik etkilerinin araştırılması ve yapı etki ilişkileri analiz çalışmaları
Özet
205 SUMMARY The Synthesis, Structure Elucidation, Antimicrobial Activity and Quantitative Structure-Activity Relationship Analysis of Some Novel 2-Benzyl-5- Substitutedbenzosazole Derivatives In this research, 23 compounds for the first time were synthesized, their in vitro antimicrobial activities were determined and their quantitative structure-activity relationships were studied. The compounds were synthesized by condensing of 2-Benzyl-5-aminobenzoxazoles and/or 2-(p-chlorobenzyl)-S-aminobenzoxazoles and carboxylic acid chlorides which were obtained by treating carboxylic acides with thionyl chloride. The purity of the compounds were controlled by TLC and melting points were determined. Their structures were elucidated by using IR, İH-NMR and Mass analysis methods. The antibacterial activitity of these compounds against some Gram positive bacteria such as Staphylococcus aureus ATCC 25923, Bacillus subtilis ATCC 6633, and Gram negative bacteria such as Escherichia coli ATCC 23556, Pseudomonas aeruginosa ATCC 10145 and the antifungal activitiy against the fungi Candida albicans ATCC 10231, Candida krusei ATCC 6258, Candida glabrata were determined as The Minimum Inhibitory Concentration (MIC) values. The MIC values of the derivatives were compared to some antibacterial and antifungal drugs. All of the compounds having MIC values as 3.12-200 (xg/ml were found active against E. coli, P. aeruginosa gram negative, S. aureus, B. subtilis as gram positive and C. albicans, C. krusei, C. glabrata as fungi. The quantitative structure-activity relationships (QSAR) analysis and DFT analysis of synthesized compounds were performed by using Hansen analysis method and B3LYP/6-3 lG(d,p) basic set on Gaussian-98 computer program, respectivelly. Key Words : Benzoxazole, Benzamide, Phenylacetamide, Antimicrobial effect, Antibacteial activity, Antifungal activity, Quantitative Structure-Activity Relationships, Hansen Analysis.