Long, Madeline F. published the artcileDiscovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping, Recommanded Product: Ethyl 2-mercaptopropanoate, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(22), 4999-5001, database is CAplus and MEDLINE.
This Letter details our efforts to replace the 3-amino moiety, an essential pharmacophore for M4 PAM activity in most M4 PAMs to date, within the thieno[2,3-b]pyridine core, as the β-amino carboxamide motif has been shown to engender poor solubility, varying degrees of P-gp efflux and represents a structural alert. A scaffold hopping exercise identified a novel 2,4-dimethylquinoline carboxamide core that provided M4 PAM activity and good CNS penetration without an amino moiety. In addition, MacMillan photoredox catalysis chem. was essential for construction of the 2,4-dimethylquinoline core.
Bioorganic & Medicinal Chemistry Letters published new progress about 19788-49-9. 19788-49-9 belongs to esters-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Ester, name is Ethyl 2-mercaptopropanoate, and the molecular formula is C5H10O2S, Recommanded Product: Ethyl 2-mercaptopropanoate.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics