Synthesis, Structure–activity Relationships, and Anticonvulsant Activities of 2-amino-4H-pyrido[3, 2-e][1, 3]thiazin-4-one Derivatives as Orally Active AMPA Receptor Antagonists PDF Free

Synthesis, Structure–activity Relationships, and Anticonvulsant Activities of 2-amino-4H-pyrido[3, 2-e][1, 3]thiazin-4-one Derivatives as Orally Active AMPA Receptor Antagonists PDF
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Published on 2015 by

Graphical abstract: Abstract: As part of a program aimed at discovering orally active 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonists, we screened our compound library and identified 2-[allyl(4-methylphenyl)amino]-4 H -pyrido[3, 2- e ][1, 3]thiazin-4-one (7 ) as a lead compound that inhibited kainate-induced neurotoxicity mediated by AMPA receptors in rat hippocampal cultures. Structure–activity relationship studies of a series of 2-amino-4 H -pyrido[3, 2- e ][1, 3]thiazin-4-one derivatives revealed that substituents on the phenyl ring attached to the 2-amino group and the 4 H -pyrido[3, 2- e ][1, 3]thiazin-4-one ring system play an important role in inhibitory activity against kainate-induced neurotoxicity. Several analogs bearing a phenyl group with a 4-substituent or five- or six-membered ring fused at the 3, 4-positions exhibited potent inhibitory activity against kainate-induced neurotoxicity. Further, some of these compounds exhibited significant suppression of maximal electroshock seizure in mice following oral administration. Of these compounds, 2-[(4-chlorophenyl)(methyl)amino]-4 H -pyrido[3, 2- e ][1, 3]thiazin-4-one (16i ) (YM928) demonstrated the most potent inhibitory effect with an ED50 value of 7.4 mg/kg.

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