Bartolome-Nebreda, Jose Manuel’s team published research in Journal of Medicinal Chemistry in 2013 | CAS: 16982-21-1

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Formula: C4H7NO2S

In 2013,Bartolome-Nebreda, Jose Manuel; Conde-Ceide, Susana; Delgado, Francisca; Iturrino, Laura; Pastor, Joaquin; Pena, Miguel Angel; Trabanco, Andres A.; Tresadern, Gary; Wassvik, Carola M.; Stauffer, Shaun R.; Jadhav, Satyawan; Gogi, Kiran; Vinson, Paige N.; Noetzel, Meredith J.; Days, Emily; Weaver, C. David; Lindsley, Craig W.; Niswender, Colleen M.; Jones, Carrie K.; Conn, P. Jeffrey; Rombouts, Frederik; Lavreysen, Hilde; Macdonald, Gregor J.; Mackie, Claire; Steckler, Thomas published 《Dihydrothiazolopyridone Derivatives as a Novel Family of Positive Allosteric Modulators of the Metabotropic Glutamate 5 (mGlu5) Receptor》.Journal of Medicinal Chemistry published the findings.Formula: C4H7NO2S The information in the text is summarized as follows:

Starting from a singleton chromanone high throughput screening (HTS) hit, we describe a focused medicinal chem. optimization effort leading to the identification of a novel series of phenoxymethyl-dihydrothiazolopyridone derivatives as selective pos. allosteric modulators (PAMs) of the metabotropic glutamate 5 (mGlu5) receptor. These dihydrothiazolopyridones potentiate receptor responses in recombinant systems. In vitro and in vivo drug metabolism and pharmacokinetic (DMPK) evaluation allowed us to select compound (I) for its assessment in a preclin. animal screen of possible antipsychotic activity. I was able to reverse amphetamine-induced hyperlocomotion in rats in a dose-dependent manner without showing any significant motor impairment or overt neurol. side effects at comparable doses. Evolution of our medicinal chem. program, structure activity, and properties relationships (SAR and SPR) anal. as well as a detailed profile for optimized mGlu5 receptor PAM I are described. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Formula: C4H7NO2S)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Formula: C4H7NO2S

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