Structure–activity relationship of thiopyrimidines as mGluR5 antagonists

descriptionPublicationkeyboard_double_arrow_right Article 01 May 2006 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 16, pages 2,467-2,469 (issn: 0960-894X,

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Authors: Lance G, Hammerland; Martin, Johansson; Jonas, Malmström; Jan P, Mattsson; Alexander B E, Minidis; Karolina, Nilsson; Alecia, Peterson; +3 Authors

doi: 10.1016/j.bmcl.2006.01.100

pmid: 16481165

Structure–activity relationship of thiopyrimidines as mGluR5 antagonists

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Abstract

Structure-activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity.

Related Organizations

Takeda (United States)
United States
ASTRAZENECA UK LIMITED
United Kingdom

Keywords

Thionucleosides, Molecular Structure, Receptor, Metabotropic Glutamate 5, Drug Evaluation, Preclinical, Stereoisomerism, In Vitro Techniques, Receptors, Metabotropic Glutamate, Cell Line, Rats, Structure-Activity Relationship, Pyrimidines, Liver, Microsomes, Animals, Humans

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