Hodgetts, Kevin J. published the artcileDiscovery of N-(1-Ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): An Orally Active Corticotropin Releasing Factor-1 (CRF-1) Receptor Antagonist, Application In Synthesis of 127972-00-3, the main research area is pyrazine preparation SAR CRF 1 receptor antagonist; orally active corticotropin releasing factor 1 receptor antagonist.
The design, synthesis, and structure-activity relationships of a novel series of pyrazines, acting as corticotropin releasing factor-1 (CRF-1) receptor antagonists, are described. Synthetic methodologies were developed to prepare a number of substituted pyrazine cores utilizing regioselective halogenation and chemoselective derivatization. Noteworthy, an efficient 5-step synthesis was developed for the lead compound I (NGD 98-2), which required no chromatog. Compound I was characterized as an orally bioavailable, brain penetrant, and highly selective CRF-1 receptor antagonist. Occupancy of rat brain CRF-1 receptors was quantified using ex vivo receptor occupancy assays, using both brain tissue homogenates as well as brain slices receptor autoradiog. Behaviorally, oral administration of I significantly antagonized CRF-induced locomotor activity at doses as low as 10 mg/kg and dose-dependently reduced the restraint stress-induced ACTH increases.
Journal of Medicinal Chemistry published new progress about Homo sapiens. 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Application In Synthesis of 127972-00-3.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem