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Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago-Potentiator ADX-47273

Darren W Engers, Alice L Rodriguez, Richard Williams, Alexis S Hammond, Daryl Venable, Oluwatomi Oluwatola, Gary A Sulikowski, P Jeffrey Conn, Craig W Lindsley

ChemMedChem. 2009 Apr;4(4):505-11.

PMID: 19197923

Abstract:

An iterative analogue library synthesis strategy rapidly developed comprehensive SAR for the mGluR5 ago-potentiator ADX-47273. This effort identified key substituents in the 3-position of oxadiazole that engendered either mGluR5 ago-potentiation or pure mGluR5 positive allosteric modulation. The mGluR5 positive allosteric modulators identified possessed the largest fold shifts (up to 27.9-fold) of the glutamate CRC reported to date as well as providing improved physiochemical properties.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP851881602 ADX-47273 ADX-47273 851881-60-2 Price
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