Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP |
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| Authors: | Alagille David Baldwin Ronald M Roth Bryan L Wroblewski Jarda T Grajkowska Ewa Tamagnan Gilles D |
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| Affiliation: | Department of Psychiatry, Yale University and VA Connecticut/116A2, 950 Campbell Avenue, West Haven, CT 06516, USA. |
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| Abstract: | We described the synthesis and biological evaluation of MPEP analogs functionalized at the position 3 of the phenyl ring. The results point out the limitation in the choice of a functional group at this position; the only substituents leading to retention of activity are NO(2) (IC(50)=13 nM) and CN (IC(50)=8 nM). |
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