Heteroaromatic side-chain analogs of pregabalin

As part of a program to identify the scope of substituents recognized by the α 2-δ protein, a series of heteroaromatic analogs, 2, of pregabalin, 1, has been identified that possess anticonvulsant activity in the DBA/2 mouse model. The methods of synthesis and preliminary pharmacology are discussed...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (9), p.2329-2332
Hauptverfasser:	Schelkun, Robert M., Yuen, Po-wai, Wustrow, David J., Kinsora, Jack, Su, Ti-Zhi, Vartanian, Mark G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticonvulsants - chemical synthesis Anticonvulsants - chemistry Anticonvulsants - pharmacology Anticonvulsants. Antiepileptics. Antiparkinson agents Biological and medical sciences Disease Models, Animal Drug Design Drug Evaluation, Preclinical gamma-Aminobutyric Acid - analogs & derivatives gamma-Aminobutyric Acid - chemical synthesis gamma-Aminobutyric Acid - chemistry gamma-Aminobutyric Acid - pharmacology In Vitro Techniques Medical sciences Mice Mice, Inbred DBA Molecular Structure Neuropharmacology Pharmacology. Drug treatments Pregabalin Seizures - prevention & control Stereoisomerism
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Zusammenfassung:	As part of a program to identify the scope of substituents recognized by the α 2-δ protein, a series of heteroaromatic analogs, 2, of pregabalin, 1, has been identified that possess anticonvulsant activity in the DBA/2 mouse model. The methods of synthesis and preliminary pharmacology are discussed herein. A series of heteroaromatic analogs of pregabalin has been identified that possess anticonvulsant activity in the DBA/2 mouse model. The methods of synthesis and preliminary pharmacology are discussed herein.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.06.090