Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype was written by Temple, Kayla J.;Engers, Julie L.;Long, Madeline F.;Watson, Katherine J.;Chang, Sichen;Luscombe, Vincent B.;Jenkins, Matthew T.;Rodriguez, Alice L.;Niswender, Colleen M.;Bridges, Thomas M.;Jeffrey Conn, P.;Engers, Darren W.;Lindsley, Craig W.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Name: N-(5-Bromopyridin-2-yl)-4-methylbenzenesulfonamide The following contents are mentioned in the article:
This Letter details the authors’ efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, the authors studied a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration. This study involved multiple reactions and reactants, such as N-(5-Bromopyridin-2-yl)-4-methylbenzenesulfonamide (cas: 207801-52-3Name: N-(5-Bromopyridin-2-yl)-4-methylbenzenesulfonamide).
N-(5-Bromopyridin-2-yl)-4-methylbenzenesulfonamide (cas: 207801-52-3) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the è?bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the è?bonds. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one Cé¥æ in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Name: N-(5-Bromopyridin-2-yl)-4-methylbenzenesulfonamide