Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS
Data(s) |
01/12/2009
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Resumo |
This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold. (C) 2009 Elsevier Ltd. All rights reserved. |
Identificador | |
Idioma(s) |
eng |
Direitos |
info:eu-repo/semantics/restrictedAccess |
Fonte |
Rodriguez , A L , Zhou , Y , Williams , R , Weaver , C D , Conn , P J & Lindsley , C W 2009 , ' Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS ' Bioorganic & Medicinal Chemistry Letters , vol 19 , no. 23 , pp. 6502-6506 . DOI: 10.1016/j.bmcl.2009.10.059 |
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 |