- 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
-
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]-4H-pyrido[3,2-e][1,3]thiazin-4-on
- Inami, Hiroshi,Shishikura, Jun-Ichi,Yasunaga, Tomoyuki,Ohno, Kazushige,Yamashita, Hiroshi,Kato, Kota,Sakamoto, Shuichi
-
p. 1788 - 1799
(2015/03/30)
-
- Inhibitor of kainic acid neurotoxicity and pyridothiazine derivative
-
PCT No. PCT/JP96/03339 Sec. 371 Date May 13, 1998 Sec. 102(e) Date May 13, 1998 PCT Filed Nov. 14, 1996 PCT Pub. No. WO97/17970 PCT Pub. Date May 22, 1997Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; R1, R2, R3, R4 and R5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R2 and R3 may together form a nitrogen-containing heterocyclic group which may have nitrogen atoms as another hetero atom, may be fused with a benzene ring and may have a lower alkyl group as a substituent.
- -
-
-