Felts, Andrew S.; Rodriguez, Alice L.; Morrison, Ryan D.; Blobaum, Anna L.; Byers, Frank W.; Daniels, J. Scott; Niswender, Colleen M.; Conn, P. Jeffrey; Lindsley, Craig W.; Emmitte, Kyle A. published the artcile< Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5>, Name: 4-Cyclopropylthiazol-2-amine, the main research area is pyrimidinylmethylquinolinecarboxamide preparation neg allosteric modulator glutamate receptor mGluR5; Central nervous system (CNS); G protein-coupled receptor (GPCR); Metabotropic glutamate receptor subtype 5 (mGlu(5)); Negative allosteric modulator (NAM); Quinoline.
Based on previous work that established fused heterocycles as viable alternatives for the picolinamide core of the authors’ lead series of mGlu5 neg. allosteric modulators (NAMs), the authors designed a novel series of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide mGlu5 NAMs. These new quinoline derivatives also contained carbon linkers as replacements for the diaryl ether oxygen atom common to the authors’ previously published chemotypes. Compounds were evaluated in a cell-based functional mGlu5 assay, and an exemplar analog 27 (6-(difluoro(pyrimidin-5-yl)methyl)-N-(4-methylthiazol-2-yl)quinoline-8-carboxamide) was >60-fold selective vs. the other seven mGlu receptors. Selected compounds were also studied in metabolic stability assays in rat and human S9 hepatic fractions and exhibited a mixture of P 450- and non-P 450-mediated metabolism
Bioorganic & Medicinal Chemistry Letters published new progress about Allosterism. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Name: 4-Cyclopropylthiazol-2-amine.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica