SYNTHESIS AND BACTERICIDAL ACTIVITY OF NOVEL BISPIDINONE DERIVATIVES

Abstract

Abstract. Introduction. The fact that no new anti-tuberculosis drugs have been launched on the
market in the last decades, as well as the fact that tuberculosis bacilli have special properties of sensitivity
with a change in living conditions in the human body, clarify the importance of the synthesis of new antituberculosis drugs. The experimental findings from this research enrich with the latest information on
modern chemistry of development and antibacterial activity of a promising class of chemical compounds -
bispidinone derivatives. The compound we have obtained has bactericidal activity and can become the
basis for the development of a new domestic safe drug. The aim of the work is to study the physicochemical and biological properties of novel bispidinone. Results and discussion. Bispidinone was
synthesized by Mannich condensation and further heated in an alcohol medium in the presence of
hydrochloride of hydroxylamine and pyridine and acylated to the corresponding oxime with a high yield
of 91.5%. The targeted O-benzoyloxime has been obtained with 72.2% by heating oxime. The βcyclodextrin complex of O-benzoyloxime (ТК-1) was screened for in vitro bactericidal properties.
Conclusion. The O-Benzoyloxime molecule (ТК-1) has proven to be a highly effective compound in
various experiments examining its bactericidal activity against strains of wild sensitive tuberculosis
mycobacteria. An acute toxicity study following a single subcutaneous injection in white-seeded mice
demonstrated that the new 3,7-substituted bispidinone (ТК-1) exhibited low toxicity when compared to
rifampicin, a standard anti-tuberculosis medication.