Sciact
  • EN
  • RU

Synthesis and analgesic activity of new alpha-truxillic acid derivatives with monoterpenoid fragments Научная публикация

Журнал Medicinal Chemistry Research
ISSN: 1054-2523 , E-ISSN: 1554-8120
Вых. Данные Год: 2016, Том: 25, Номер: 8, Страницы: 1608-1615 Страниц : 8 DOI: 10.1007/s00044-016-1593-z
Ключевые слова Terpenoid; Analgesic activity; Acetic acid-induced writhing test; Hot plate test
Авторы Sokolova Anastasiya 1,2 , Pavlova Alla 1 , Komarova Nina 1 , Ardashov Oleg 1 , Shernyukov Andrey 1 , Gatilov Yuriy 1 , Yarovaya Olga 1,2 , Tolstikova Tat'yana 1,2 , Salakhutdinov Nariman 1,2
Организации
1 (Данные Web of science) Russian Acad Sci, Siberian Branch, NN Vorozhtzov Novosibirsk Inst Organ Chem, Lavrenteva Ave 9, Novosibirsk 630090, Russia
2 (Данные Web of science) Novosibirsk State Univ, Pirogova St 2, Novosibirsk 630090, Russia

Реферат: Novel derivatives of alpha-truxillic acid with a camphor framework were synthesized and evaluated for their in vivo analgesic activity. alpha-Truxillic acid derivatives were prepared via solvent-free photocatalyzed [2+2] cyclodimerization of (E)-cinnamic acid. Target compounds were obtained through the substitution of -Cl or -OH groups in alpha-truxillic acid. The chemical structures of the synthesized compounds were elucidated by H-1, C-13-NMR, and mass spectrometry. Their analgesic activities were evaluated by the acetic acid-induced writhing test and the hot plate method. Compounds 7b and 7f containing the cyclobutane unit and natural fragments at 10 mg/kg exhibited analgesic activity in the acetic acid-induced writhing test, while alpha-truxillic acid (10 mg/kg, per os) did not show analgesic activity in the test. Intermediate 2 caused a decrease in the writhing with pain inhibition of 28 %. In the hot plate test, borneol showed high analgesic activity with pain inhibition of 60 %.
Библиографическая ссылка: Sokolova A. , Pavlova A. , Komarova N. , Ardashov O. , Shernyukov A. , Gatilov Y. , Yarovaya O. , Tolstikova T. , Salakhutdinov N.
Synthesis and analgesic activity of new alpha-truxillic acid derivatives with monoterpenoid fragments
Medicinal Chemistry Research. 2016. V.25. N8. P.1608-1615. DOI: 10.1007/s00044-016-1593-z WOS Scopus РИНЦ OpenAlex
Даты:
Опубликована online: 17 мая 2016 г.
Опубликована в печати: 1 авг. 2016 г.
Идентификаторы БД:
Web of science: WOS:000381207600008
Scopus: 2-s2.0-84969221111
РИНЦ: 1608
OpenAlex: W2403671372
Цитирование в БД:
БД Цитирований
Web of science 17
Scopus 18
OpenAlex 18
Альметрики: