Cid, Jose Maria published the artcileDiscovery of 1,4-Disubstituted 3-Cyano-2-pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor, Category: chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2012), 55(5), 2388-2405, database is CAplus and MEDLINE.
The discovery and characterization of compound 48, a selective and in vivo active mGlu2 receptor pos. allosteric modulator (PAM), are described. A key to the discovery was the rational exploration of the initial HTS hit 13 guided by an overlay model built with reported mGlu2 receptor PAM chemotypes. The initial weak in vitro activity of the hit 13 was quickly improved, although compounds still had suboptimal druglike properties. Subsequent modulation of the physicochem. properties resulted in compounds having a more balanced profile, combining good potency and in vivo pharmacokinetic properties. Final refinement by addressing cardiovascular safety liabilities led to the discovery of compound (I). Besides good potency, selectivity, and ADME properties, I displayed robust in vivo activity in a sleep-wake EEG (sw-EEG) assay consistent with mGlu2 receptor activation, in accordance with previous work from our laboratories
Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Category: chlorides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics