Синтез и антибактериальная активность тетразольных производных хитина

The present study is devoted to the synthesis and study of the antibacterial activity in vitro of new tetrazole derivatives of natural polymer chitin of high, medium and low molecular weights with high, medium and low degree of substitution. The results showed that the obtained tetrazole derivatives are characterized by pronounced antibacterial activity in vitro against both S. aureus and E. coli strains. Among all derivatives, the highest antibacterial activity is demonstrated by a tetrazole derivative of chitin of moderate molecular weight and moderate degree of substitution. The antibacterial activity of this derivative as measured by the zone of inhibition of bacterial growth is comparable to the antibacterial activity of reference antibiotics ampicillin and gentamicin.Настоящее исследование посвящено синтезу и изучению антибактериальной активности in vitro новых тетразольных производных природного полимера хитина высоких, средних и низких молекулярных масс с высокими, средними и низкими степенями замещения. Полученные тетразольные производные характеризуются выраженной антибактериальной активностью in vitro в отношении S. aureus и E. coli. Среди всех полученных производных наибольшей антибактериальной активностью характеризуется производное хитина средней молекулярной массы умеренной степени замещения. Установленная по зоне ингибирования роста бактерий антибактериальная активность данного производного сопоставима с антибактериальной активностью антибиотиков ампициллина и гентамицина

Synthesis and Antibacterial Activity of Chitin Tetrazole Derivatives

New tetrazole derivatives of natural chitin polymers of high, medium, and low molecular masses with high, medium, and low degrees of substitution were synthesized and tested in vitro for antibacterial activity. The obtained tetrazole derivatives were characterized by pronounced antibacterial activity in vitro against S. aureus and E. coli. The chitin derivative of medium molecular mass with a medium degree of substitution had the highest antibacterial activity among all obtained derivatives. The antibacterial activity of this derivative as measured by bacterial growth inhibition zones was comparable to those of the antibiotics ampicillin and gentamycin. © 2020, Springer Science+Business Media, LLC, part of Springer Nature

Novel non-toxic high efficient antibacterial azido chitosan derivatives with potential application in food coatings

In this work, we developed a simple method for the preparation of N-(3-azido-2-hydroxypropyl)chitosan. We compared the antibacterial activity of N-(3-azido-2-hydroxypropyl)chitosans and previously synthesized N-(2-azidoethyl)chitosans. N-(3-azido-2-hydroxypropyl)chitosans possess higher antibacterial effect which is comparable with that of ampicillin and gentamicin. The effect is due to azido pharmacophore –CH2–CH(OH)–CH2–N3 (for N-(3-azido-2-hydroxypropyl)chitosan) or –CH2–CH2–N3 (for N-(2-azidoethyl)chitosan) introduced in chitosan chain, since the corresponding organic azides NH2–CH2–CH2–N3 and NH2–CH2–CH2–N3 are characterized by high antibacterial activity. However, high antibacterial organic azides NH2–CH2–CH2–N3 and NH2–CH2–CH2–N3 are characterized by high toxicity. Their conjugation to the chitosan chain saves their antibacterial effect, but strongly diminishes their toxicity, and the toxicity of the resulting derivatives is comparable with that of the starting chitosan. These findings are of interest to food science, since novel effective food coatings can be developed on basis of prepared derivatives. © 201