Peculiarities of Pharmacological Activity of Tetrahydropyridone and Hexahydroquinoline Derivatives in Experiment

Аннотация

Introduction: Due to widespread inflammatory processes, often accompanied by pain and fever syndromes, NSAIDs are now the most prescribed drug group in the world. NSAIDs are characterized by taking a leading position in the number and severity of adverse actions. In recent decades, the efforts of scientists have been aimed at seaching for adequate ways to increase the safety profile of NSAIDs.

Materials and methods: In a series of experiments, the main objects of research were derivatives of α-cyanothioacet­amide – new tetrahydropyridones under laboratory codes TD 0364, TD 0353, TD 0351, CV 036, as well as hexahydro­quinolines CV 125 and OCO 5184. One promising area for searching for effective and safe pharmacological agents is some derivatives of α-cyanothioacetamide (CAS Number: 7357-70-2). The trigeminal orofacial pain test and the ther­mal tail immersion test were used to assess the analgesic effect. Determination of antipyretic activity was carried out on the yeast-fever model. To study an anti-inflammatory activity, the method of subacute non-infectious parotitis was used.

Results and discussion: The results of the experiment made it possible to find among the new samples of tetrahydro­pyridones and hexahydroquinolines the compounds with analgesic, anti-inflammatory and antipyretic activities, which, in terms of these types of activities in dynamics, surpass the reference (paracetamol, diclofenac sodium, and ketorolac). It is important that these compounds have low acute toxicity.

Conclusion: The consequence of the above is the necessity of further preclinical and clinical studies of samples of α-cyanothioacetamide derivatives in order to create new promising highly effective and safe drugs with analgesic, anti-inflammatory and antipyretic activities.