23844-57-7Relevant academic research and scientific papers
Design, Synthesis, and Pharmacological Evaluation of Novel β2/3 Subunit-Selective γ-Aminobutyric Acid Type A (GABAA) Receptor Modulators
Stadler, Marco,Monticelli, Serena,Seidel, Thomas,Luger, Denise,Salzer, Isabella,Boehm, Stefan,Holzer, Wolfgang,Schwarzer, Christoph,Urban, Ernst,Khom, Sophia,Langer, Thierry,Pace, Vittorio,Hering, Steffen
, p. 317 - 341 (2018/11/02)
Subunit-selective modulation of γ-aminobutyric acid type A receptors (GABAAR) is considered to exert fewer side effects compared to unselective clinically used drugs. Here, the β2/3 subunit-selective GABAAR modulators valerenic acid (VA) and loreclezole (LOR) guided the synthesis of novel subunit-selective ligands with simplified structures. We studied their effects on GABAARs expressed in Xenopus laevis oocytes using two-microelectrode voltage clamp technique. Five compounds showed significantly more efficacious modulation of GABA-evoked currents than VA and LOR with retained potency and selectivity. Compound 18 [(E)-2-Cyano-3-(2,4-dichlorophenyl)but-2-enamide] induced the highest maximal modulation of GABA-induced chloride currents (Emax: 3114 ± 242%), while 12 [(Z)-3-(2,4-dichlorophenyl)but-2-enenitrile] displayed the highest potency (EC50: 13 ± 2 μM). Furthermore, in hippocampal neurons 12 facilitated phasic and tonic GABAergic inhibition, and in vivo studies revealed significantly more potent protection against pentylenetetrazole (PTZ)-induced seizures compared to VA and LOR. Collectively, compound 12 constitutes a novel, simplified, and subunit-selective GABAAR modulator with low-dose anticonvulsant activity.
A phenoxy carboxylic acid ester herbicide preparation method (by machine translation)
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, (2019/01/08)
The invention provides a phenoxy carboxylic acid ester herbicide preparation method, including: S1, phenol in the presence of alkaline substance with the chlorinated carboxylic acid ester condensation reaction, phenoxy carboxylic acid ester obtained; the ClR states the chloro- carboxylic acid ester of the general formula1 COOR, R1 Is C1 - 3 alkylene or alkylidene, R is C1 - 10 alkyl or C3 - 10 cycloalkyl; S2, the [...] ester in the 1st and 2nd catalyst the presence of a catalyst, with the chlorinating agent to carry out the selective chlorination of, get [...] ester; the Lewis acid catalyst is selected from the 1st, the 2nd catalyst is C5 - 22 of the thioether, thiazole, thiophene compounds or different benzisothiazoles; S3, will the [...] ester with an alcohol reaction, as shown in formula I phenoxy carboxylic acid ester herbicide; R3 Is H, Cl or CH3 , R ' is a C4 - 20 alkyl or cycloalkyl. This invention can improve the product quality and the production environment, three waste low. (by machine translation)
Enzyme catalysed hydrolysis of chlorophenoxypropionates
Chenevert, Robert,D'Astous, Linda
, p. 1219 - 1222 (2007/10/02)
We report on the enzymatic hydrolysis of methyl 2-phenoxypropionate and of the following chlorinated derivatives: methyl o-chloro-, m-chloro-, p-chloro-, and o,p-dichloro-2-phenoxypropionates. α-Chymotripsyn, lipase, and pig liver esterase have an R enantioselectivity whereas subtilisin has an S enantioselectivity.Enantiomeric excess (e.e.) cover a wide range (from 5 to 100percent).
