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3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators.

Zhang, Lei; Rogers, Bruce N; Duplantier, Allen J; McHardy, Stanley F; Efremov, Ivan; Berke, Helen; Qian, Weimin; Zhang, Andy Q; Maklad, Noha; Candler, John; Doran, Angela C; Lazzaro, John T; Ganong, Alan H.

Bioorg Med Chem Lett ; 18(20): 5493-6, 2008 Oct 15.

Article in English | MEDLINE | ID: mdl-18812259

ABSTRACT

The synthesis and structure-activity relationship (SAR) of a novel series of 3-(imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers, derived from a high throughput screening (HTS), are described. Subsequent optimization led to identification of potent, metabolically stable and orally available mGluR2 positive allosteric modulators (PAMs).

Subject(s)

Allosteric Regulation , Azabicyclo Compounds/chemical synthesis , Benzimidazoles/chemical synthesis , Chemistry, Pharmaceutical/methods , Ethers/chemistry , Receptors, Metabotropic Glutamate/chemistry , Administration, Oral , Allosteric Site , Animals , Azabicyclo Compounds/pharmacology , Benzimidazoles/pharmacology , Drug Design , Drug Evaluation, Preclinical , Humans , Microsomes/drug effects , Models, Chemical , Rats , Schizophrenia/drug therapy , Structure-Activity Relationship

ABSTRACT

Subject(s)

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