Реферат: In this paper, new thiazolidinones, thiazinanones, and thiazolidinediones based on a monoterpenoid (-)-campholenic aldehyde were synthesized and their antiulcer and anti-inflammatory activity was investigated. The thiazolidinones and thiazinanones containing a (-)-campholenic moiety have been shown to possess antiulcerogenic properties in indomethacin-induced ulcer test comparable to the activity of the reference drug omeprazole. None of the investigated thiazolidinediones showed antiulcerative activity in the test. One of the (-)-campholenic aldehyde-derived thiazolidinones has also demonstrated high anti-inflammatory activity on the histamine-induced inflammatory edema model similar to the activity of diclofenac. It is shown that changing a (-)-campholenic substituent for a linear aliphatic or a terpenic fragment with a pinane scaffold results in decreasing the pharmacological properties, though the (-)-campholenic moiety does not seem to make a key contribution to the pharmacological activity. Compounds 11 and 17 have been shown to exhibit antiulcer and anti-inflammatory action at a dose of 100 mg/kg. © 2021, Institute of Chemistry, Slovak Academy of Sciences.

Библиографическая ссылка: Borisova M.S. , Ivankin D.I. , Sokolov D.N. , Luzina O.A. , Rybalova T.V. , Tolstikova T.G. , Salakhutdinov N.F.
Synthesis, antiulcerative, and anti-inflammatory activities of new campholenic derivatives-1,3-thiazolidin-4-ones, 1,3-thiazolidine-2,4-diones, and 1,3-thiazinan-4-ones
Chemical Papers. 2021. V.75. P.5503–5514. DOI: 10.1007/s11696-021-01741-5 WOS Scopus РИНЦ

Даты:

Опубликована online:

18 июн. 2021 г.

Идентификаторы:

Web of science	WOS:000662874100002
Scopus	2-s2.0-85108065239
РИНЦ	46819065
OpenAlex	W3177162844

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