TY - JOUR AU - MALMAKOVA, AIGUL YE. AU - YU, VALENTINA K. AU - PRALIYEV, KALDYBAY D. AU - KALDYBAYEVA, ALTYNAI B. AU - AMIRKULOVA, MARZHAN K. PY - 2021/01/31 Y2 - 2024/03/29 TI - SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF NOVEL BISPIDINE DERIVATIVES JF - International Journal of Applied Pharmaceutics JA - Int J App Pharm VL - 13 IS - 1 SE - Full Proceeding Paper DO - 10.22159/ijap.2021.v13s1.Y1013 UR - https://journals.innovareacademics.in/index.php/ijap/article/view/40954 SP - 69-74 AB - <p><strong>Objective</strong>: Derivatives of 3,7-diazabicyclo[3.3.1]nonan-9-one attract considerable attention from pharmacists for the treatment of a wide range<br>of diseases. According to this interest, the novel derivatives of 3-cyclopropanmethyl-7-alkoxyalkyl-3,7-diazabicyclo[3.3.1]nonan-9-one with<br>isopropoxypropyl and ethoxypropyl substituents in the position 7 had been synthesized to study their biological activity and toxicity. The practical<br>significance of the work is in the accumulation and development of scientific representations about diazabicyclic compounds, methods for their<br>synthesis, structure, and properties, which can subsequently be used in a targeted design and identification of even more complex systems, as well<br>as in the development of further research in the field of 3,7-diazabicyclo[3.3.1]nonanes. For this purpose, complexes of the synthesized compounds<br>with β-cyclodextrin are obtained and their biological activity is investigated at the Department of Pharmacology of S.D. Asfendiyarov Kazakh National<br><strong>Medical</strong> University with the aid of the pharmacological tests.<br>Methods: An experimental study of local anesthetic activity on the models of infiltration, conduction anesthesia, and acute toxicity of synthesized<br>molecules was carried out using primary screening methods.<br><strong>Results</strong>: As a result of pharmacological screening, it has been found that the compounds exhibit local anesthetic activity and low toxicity and was<br>recommended for in-depth study of their pharmacological properties.<br><strong>Conclusion</strong>: It turned out that a nature of the N-alkoxyalkyl radical does not affect the toxicity of cyclopropanmethyl- substituted bispidines. In the<br>series of O-benzoyloximes of bispidinones, the isopropoxypropyl- substituted analog is 1.3 times less toxic than ethoxypropyl- one.</p> ER -