In 2015,Burdi, Douglas F.; Campbell, John E.; Wang, Jun; Zhao, Sufang; Zhong, Hua; Wei, Jianfeng; Campbell, Una; Shao, Liming; Herman, Lee; Koch, Patrick; Jones, Philip G.; Hewitt, Michael C. published 《Evolution and synthesis of novel orally bioavailable inhibitors of PDE10A》.Bioorganic & Medicinal Chemistry Letters published the findings.Application of 16982-21-1 The information in the text is summarized as follows:
The design and synthesis of highly potent, selective orally bioavailable inhibitors of PDE10A is reported. Starting with an active compound of modest potency from a small focused screen, we were able to evolve this series to a lead mol. with high potency and selectivity vs. other PDEs using structure-based design. A systematic refinement of ADME properties during lead optimization led to a lead compound with good half-life that was brain penetrant. Compound I was highly potent vs. PDE10A (IC50 = 1.0 nM), demonstrated high selectivity (>1000-fold) against other PDEs and was efficacious when dosed orally in a rat model of psychosis, PCP-induced hyperlocomotion with an EC50 of 1 mg/kg. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Application of 16982-21-1)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Application of 16982-21-1
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Ester – Wikipedia,
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