Wim Dehaen, together with colleagues from JU Leuven and Kazakhstan, has a new article on the synthesis and investigation of the biological activity of a number of new betulonic acid derivatives containing 1,2,3-triazole fragments. A version of the article that has not been peer reviewed can be accessed on the preprints.org website.
A number of chemical modifications were carried out in order to synthesize new compounds based on the triterpenoid betulonic acid. Triazolation reactions were carried out for the synthesis of new 1,2,3-triazole derivatives based on betulonic acid. Chemical changes were made on the carbonyl group at the C-3 position of the initial molecule and on the carboxyl and hydroxyl groups at the C-28 position. Chromatographic methods were used to separate and purify the formed products. Spectroscopic (NMR-, mass-) methods were used to establish the structure of synthesized compounds. As a result of the chemical transformations carried out, a number of new derivatives of betulonic acid were obtained. All synthesized compounds were tested for antimicrobial and cytotoxic activity. As a result, compounds with pronounced antimicrobial activity were identified.
Reference
https://www.preprints.org/manuscript/202406.0465/v1
Acknowledgement
The authors thank the staff for technical support with NMR and for technical assistance with mass spectrometry.
