Physicochemical parameters and the diuretic activity of 5-(4-R)behzyl-1,3,4-oxadiazol-2-il-thioacetic acid amides
DOI:
https://doi.org/10.24959/nphj.15.2024Keywords:
1, 3, 4-oxadіazol, concept of «drug likeness», Lipinski’s Rule of Five, diuretic activity, cytotoxicityAbstract
The group of aryl(heteryl)amides of 5-(4-R)benzyl-1,3,4-oxadіazol-2-il-thioacetic acid has been tested for compliance with the “drug likeness” concept. A number of physical and chemical properties that determine bioavailability according to Lipinski’s Rule of Five has been calculated using the ACD/ Labs computer programme. It has been found that these compounds can be recommended for further research as compounds with favourable physicochemical properties according to Lipinski’s Rule of Five. The results of the experimental study of the ability of new substances to stimulate the urinary renal function predicted by the computer PASS programme have shown that some of the new compounds synthesized are promising diuretics. The results of studying cytotoxicity in vitro for the most promising compounds have shown that these compounds possess low toxicity. The pharmacological screening has allowed to select two promising compounds that are relevant for further study.References
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