Structure—Activity Relationship of Local Anesthetics Based on Alkynylpiperidine Derivatives
Zhumakova S.S. Malmakova A.E. Yu V.K. Praliev K.D. Iskakova T.K. Ten A.Y. Amirkulova M.K. Kadyrova D.M. Satpaeva E.M. Seilkhanov T.M.
March 2021Springer
Pharmaceutical Chemistry Journal
2021#54Issue 121209 - 1214 pp.
The influence of the nature of the acyl (propionyl and benzoyl) moiety and the piperidine ring C4 substituent on the activity of several alkynylpiperidine derivatives was studied. The presence of an alkyl (hexyl) radical on the triple bond of the piperidine ring C4 substituent in the infiltration anesthesia model had a positive effect on the anesthesia index and the duration of both total and general anesthesia as compared to lidocaine, novocaine, and trimecaine taken as reference drugs. The ester of 4-(octyn-1-yl)piperidol-1-propionic acid was the most active anesthetic among the studied compounds. Modification of the triple bond (exhaustive hydrogenation and hydration) led to a decrease in the duration of anesthesia. The activity of the benzoate was greater than that of the propionate in the propionate-benzoate pair.
alkynylpiperidine , anesthetic , benzoates , propionates , toxicity
Text of the article Перейти на текст статьи
A. B. Bekturov Institute of Chemical Sciences, Almaty, 050010, Kazakhstan
K. I. Satbayev University, Almaty, 050013, Kazakhstan
S. D. Asfendiyarov Kazakh National Medical University, Almaty, 050000, Kazakhstan
Sh. Ualikhanov Kokshetau State University, Kokshetau, 020000, Kazakhstan
A. B. Bekturov Institute of Chemical Sciences
K. I. Satbayev University
S. D. Asfendiyarov Kazakh National Medical University
Sh. Ualikhanov Kokshetau State University
10 лет помогаем публиковать статьи Международный издатель
Книга Публикация научной статьи Волощук 2026 Book Publication of a scientific article 2026