Davoren, Jennifer E. published the artcileDesign and optimization of selective azaindole amide M1 positive allosteric modulators, Application In Synthesis of 19959-71-8, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(2), 650-655, database is CAplus and MEDLINE.
Selective activation of the M1 receptor via a pos. allosteric modulator (PAM) is a new approach for the treatment of the cognitive impairments associated with schizophrenia and Alzheimer’s disease. A novel series of azaindole amides and their key pharmacophore elements are described. The nitrogen of the azaindole core is a key design element as it forms an intramol. hydrogen bond with the amide N-H thus reinforcing the bioactive conformation predicted by published SAR and the authors’ homol. model. Representative compound 25 is a potent and selective M1 PAM that has well aligned physicochem. properties, adequate brain penetration and pharmacokinetic (PK) properties, and is active in vivo. These favorable properties indicate that this series possesses suitable qualities for further development and studies.
Bioorganic & Medicinal Chemistry Letters published new progress about 19959-71-8. 19959-71-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Pyridine, name is 4-(1H-Pyrazol-4-yl)pyridine, and the molecular formula is C8H7N3, Application In Synthesis of 19959-71-8.
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