SYNTHESIS AND EXPERIMENTAL STUDY OF THE LOCAL ANESTHETIC ACTIVITY OF NEW MODIFIED PIPERAZINE DERIVATIVES
Khaiitova M. Seitaliyeva A. Smagulova G. Ten A. Yu V. Satbayeva E.
January 2023Romanian Society for Pharmaceutical Sciences
Farmacia
2023#71Issue 1154 - 164 pp.
N-substituted piperazines, an important class of compounds with different pharmacological activities were taken as the basic starting object for the synthesis and study of α-aminophosphonates. The objective of the study was the synthesis, analysis of biological effects (toxicity and local anaesthetic activity) of some new piperazine derivatives, and the evaluation of their potential pharmacological effects. The new piperazine derivatives were coded as LAS-276, LAS-277, LAS-278, where LAS is a local anaesthetic substance. The compounds were synthesized under the conditions of the Kabachnik-Fields reaction. Their acute toxicity in mice, the local anaesthetic activity in a regional and infiltration anaesthesia models were studied, and their estimated pharmacological activity was analysed using the online PASS (Prediction of Activity Spectra for Substances) program. In a series of experiments the administration of high doses of the studied compounds has not caused death of laboratory animals. The study of local anaesthetic activity in the infiltration anaesthesia model showed varying degrees of activity. The compounds showed moderate activity on the regional anaesthesia model. The PASS analysis revealed a very high probability of thrombolytic, anticoagulant, antisclerotic effects and stimulation of endothelin receptors. The implemented studies revealed the low toxicity, moderate local anaesthetic activity of the studied piperazine compounds. There is also a high probability of their thrombolytic activity, which requires further research.
computer screening , local anesthetic activity , piperazines , toxicity
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Department of Pharmacology, Asfendiyarov Kazakh National Medical University, Almaty, Kazakhstan
Department of Fundamental Medicine, Аl-Farabi Kazakh National University, Almaty, Kazakhstan
Laboratory of Synthetic and Natural Medicinal Compounds Chemistry, Bekturov Institute of Chemical Sciences, Almaty, Kazakhstan
Department of Pharmacology
Department of Fundamental Medicine
Laboratory of Synthetic and Natural Medicinal Compounds Chemistry
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