Synthetic Transformations of Higher Terpenoids. 39.∗ Synthesis and Analgesic Activity of Isopimaric Acid Derivatives Full article
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Chemistry of Natural Compounds
ISSN: 0009-3130 , E-ISSN: 1573-8388 |
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| Output data | Year: 2021, Volume: 57, Pages: 474–481 Pages count : DOI: 10.1007/s10600-021-03391-1 | ||
| Tags | amides; analgesic activity; diterpenoids; esters; isopimaric acid | ||
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Abstract:
New derivatives of isopimaric acid at the carboxylic acid were prepared. Their analgesic activity was studied in models of visceral and thermal pain. Isopimaric acid amides with aminoethanol and (2R)-(hydroxymethyl)pyrrolidine groups exhibited statistically significant analgesic activity in acetic acid-induced writhing (5 and 25 mg/kg doses) and hot-plate tests (25 mg/kg dose) that was comparable to that of diclofenac sodium (10 mg/kg dose). The new agents were characterized by low (LD50 > 1250 mg/kg) in vivo toxicity. Molecular modeling of possible interaction of the most active compounds with transmembrane G-protein-binding cannabinoid receptor CB2 was performed. © 2021, Springer Science+Business Media, LLC, part of Springer Nature.
Cite:
Gromova M.A.
, Kharitonov Y.V.
, Borisov S.A.
, Baev D.S.
, Tolstikova T.G.
, Shul’ts E.E.
Synthetic Transformations of Higher Terpenoids. 39.∗ Synthesis and Analgesic Activity of Isopimaric Acid Derivatives
Chemistry of Natural Compounds. 2021. V.57. P.474–481. DOI: 10.1007/s10600-021-03391-1 WOS Scopus РИНЦ OpenAlex
Synthetic Transformations of Higher Terpenoids. 39.∗ Synthesis and Analgesic Activity of Isopimaric Acid Derivatives
Chemistry of Natural Compounds. 2021. V.57. P.474–481. DOI: 10.1007/s10600-021-03391-1 WOS Scopus РИНЦ OpenAlex
Dates:
| Published print: | May 1, 2021 |
| Published online: | May 28, 2021 |
Identifiers:
| Web of science: | WOS:000655545100001 |
| Scopus: | 2-s2.0-85106699876 |
| Elibrary: | 46777062 |
| OpenAlex: | W3167519125 |