Development of effective methods for the synthesis of azole compounds based on natural substances with antibacterial, anti-inflammatory and antioxidant effects

New Materials Research Institute

Scientific supervisor – Candidate of Chemical Sciences, acting Associate Professor of the Department of Ch&ChT Rakhimberdinova Zh.B.

Relevance

To date, there is little information about chemical synthesis methods for the introduction of azole heterocycles into the structure of natural compounds, in particular alkaloids, which has determined the relevance and prospects of their study for the search for new bioactive compounds.

Project objective

Development of effective methods for the synthesis of azole compounds based on natural substances with antibacterial, anti-inflammatory and antioxidant effects, serving as new medicinal properties, as well as full establishment of their structure and bioscreening of synthesized compounds using the PASS program.

Expected and achieved results

Methods for obtaining and optimal conditions for the synthesis of azole derivatives based on the cytisine alkaloid and biogenic amines have been developed. Methods for the preparation of pyrazoles and oxazoles based on the alkaloid cytisine and biogenic amines morpholine and piperidine and their chemical modification have been developed. Possible mechanisms of reactions of their formation are investigated, the structure of new compounds is established. Bioscreening of new synthesized substances was carried out.

Methods of obtaining and optimal conditions for the synthesis of oxozoline derivatives of the cytisine alkaloid under the conditions of classical synthesis of microwave and ultrasonic activation have been developed, the structure and their biological activity have been established. By heterocyclization of the obtained amino alcohol derivatives of the alkaloid cytisine and biogenic amines, oxazole derivatives were obtained. Bioscreening of synthesized substances was carried out.

The developed methods for obtaining potentially biologically active azoles are recommended for the development of new biologically active substances and practical application in the synthesis of these classes of compounds.