Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 13, 2007, Pages 3769-3773

  Zhang, Jiange ^a   Zhang, Pei ^a   Liu, Xianbo ^a   Fang, Kai ^b   Lin, Guoqiang ^b  

^a ZHENGZHOU UNIVERSITY   (China)

^b SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY   (China)

Author keywords

(R) N (Diarylmethylthio sulfinyl)ethyl propyl piperidine carboxylic acid derivatives; Antiepileptic; GABA uptake inhibitors; GAT1

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID CARRIER; GUVACINE; NIPECOTIC ACID; PIPERIDINE DERIVATIVE; TIAGABINE; TRITIUM;

4 AMINOBUTYRIC ACID UPTAKE; ARTICLE; CELL LINE; DRUG ACTIVITY; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; INHIBITION KINETICS; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTICONVULSANTS; CARBOXYLIC ACIDS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; GABA ANTAGONISTS; GABA PLASMA MEMBRANE TRANSPORT PROTEINS; GAMMA-AMINOBUTYRIC ACID; IMIDAZOLES; INHIBITORY CONCENTRATION 50; MICE; MODELS, CHEMICAL; NIPECOTIC ACIDS; PIPERIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; TEMPERATURE;

EID: 34250221170     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.010     Document Type: Article

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19. 2S + H: 426.2466620, found: 426.2461265.
20. 2S + H: 440.2619260, found: 440.2617766.
21. 2S - H: 432.17739, found: 432.17695.
22. 2S - H: 446.1923390, found: 446.1926013.
23. 3S - H: 448.17141, found: 448.17187.