Article

Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.

Gedeon Richter Plc, Budapest, Hungary.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 08/2010; 20(15):4371-5. DOI:10.1016/j.bmcl.2010.06.075 pp.4371-5
Source: PubMed

ABSTRACT Hit-to-lead optimization of a HTS hit led to new carbamoyloxime derivatives. After identification of an advanced hit (8d) the CYP enzyme inhibitory activity of this class of compounds was successfully eliminated. Systematic exploration of different parts of the advanced hit led us to some promising lead compounds with mGluR5 affinities comparable to that of MPEP.

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Keywords

CYP enzyme inhibitory activity
 
different parts
 
mGluR5 affinities comparable
 
MPEP
 
Systematic exploration