Synthesis and SAR of centrally active mGlu(5) positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold
| Data(s) |
01/03/2011
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| Resumo |
This Letter describes the hit-to-lead progression and SAR of a series of biphenyl acetylene compounds derived from an HTS screening campaign targeting the mGlu(5) receptor. 'Molecular switches' were identified that modulated modes of pharmacology, and several compounds within this series were shown to be efficacious in reversal of amphetamine induced hyperlocomotion in rats after ip dosing, a preclinical model that shows similar positive effects with known antipsychotic agents. Published by Elsevier Ltd. |
| Identificador | |
| Idioma(s) |
eng |
| Direitos |
info:eu-repo/semantics/restrictedAccess |
| Fonte |
Williams , R , Manka , J T , Rodriguez , A L , Vinson , P N , Niswender , C M , Weaver , C D , Jones , C K , Conn , P J , Lindsley , C W & Stauffer , S R 2011 , ' Synthesis and SAR of centrally active mGlu(5) positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold ' Bioorganic & Medicinal Chemistry Letters , vol 21 , no. 5 , pp. 1350-1353 . DOI: 10.1016/j.bmcl.2011.01.044 |
| Palavras-Chave | #/dk/atira/pure/subjectarea/asjc/3000/3003 #Pharmaceutical Science #/dk/atira/pure/subjectarea/asjc/3000/3002 #Drug Discovery #/dk/atira/pure/subjectarea/asjc/1600/1605 #Organic Chemistry #/dk/atira/pure/subjectarea/asjc/1300/1313 #Molecular Medicine #/dk/atira/pure/subjectarea/asjc/1300/1312 #Molecular Biology #/dk/atira/pure/subjectarea/asjc/1300/1308 #Clinical Biochemistry #/dk/atira/pure/subjectarea/asjc/1300/1303 #Biochemistry |
| Tipo |
article |
