Bai, Yajun’s team published research in European Journal of Medicinal Chemistry in 183 | CAS: 16909-09-4

European Journal of Medicinal Chemistry published new progress about 16909-09-4. 16909-09-4 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Benzene,Ether, name is (E)-3-(2,4-Dimethoxyphenyl)acrylic acid, and the molecular formula is C11H12O4, Synthetic Route of 16909-09-4.

Bai, Yajun published the artcilePolygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic ¦Á-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study, Synthetic Route of 16909-09-4, the publication is European Journal of Medicinal Chemistry (2019), 111650, database is CAplus and MEDLINE.

Inspired by the traditional Chinese herbal pair of Polygala tenuifolia-Acori Tatarinowii for treating epilepsy, 33 novel substituted cinnamic ¦Á-asaronol esters and analogs, I [R = 2-, 3-, 4-OMe, 2,3-(MeO)2, 2,3,5-(MeO)3, 2,3,4,5,6-(MeO)5, 4-Br, 3-CF3, etc.], II, III, and IV, were designed by Combination of Traditional Chinese Medicine Mol. Chem. (CTCMMC) strategy, synthesized and tested systematically not only for anticonvulsant activity in three mouse models but also for lactate dehydrogenase (LDH) inhibitory activity. Thus, compounds I [R = 3,4,5-(MeO)3, 2,3,4,5-(MeO)4, 2,3,4,6-(MeO)4, 4-F] (V) displayed excellent and broad spectra of anticonvulsant activities with modest ability in preventing neuropathic pain, as well as low neurotoxicity. The protective indexes of these four compounds compared favorably with stiripentol, lacosamide, carbamazepine and valproic acid. 68-70 exhibited good LDH1 and LDH5 inhibitory activities with noncompetitive inhibition type, and were more potent than stiripentol. Compounds V exhibited good LDH1 and LDH5 inhibitory activities with noncompetitive inhibition type, and were more potent than stiripentol. Notably, I [R = 2,3,4,6-(MeO)4], as a representative agent, was also shown as a moderately pos. allosteric modulator at human ¦Á1¦Â2¦Ã2 GABAA receptors (EC50 46.3 ¡À 7.3 ¦ÌM). Thus, I [R = 3,4,5-(MeO)3, 2,3,4,5-(MeO)4, 2,3,4,6-(MeO)4] were promising candidates for developing into anti-epileptic drugs, especially for treatment of refractory epilepsies such as Dravet syndrome.

European Journal of Medicinal Chemistry published new progress about 16909-09-4. 16909-09-4 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Benzene,Ether, name is (E)-3-(2,4-Dimethoxyphenyl)acrylic acid, and the molecular formula is C11H12O4, Synthetic Route of 16909-09-4.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia