Bioorganic and Medicinal Chemistry Letters p. 771 - 774 (2002)
Update date:2022-08-03
Topics:
Fujita, Masakazu
Seki, Taketsugu
Inada, Haruaki
Shimizu, Kazuhiro
Takahama, Akane
Sano, Tetsuro
Compounds 1 or 2 which possess dual-acting PAF antagonist/TxSI in a previous paper were modified and evaluated for the dual-acting activity. It was found that several compounds were potent dual-acting PAF antagonist/TxSI in and ex vivo. 6-(2-Chlorophenyl)-3-[4-[(E/Z)-6-ethoxycarbonyl-1-(3-pyridyl)-1- hexenyl]phenylmethyl]-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido[4′, 3′: 4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine (12) is excellent orally dual-acting PAF antagonist/TxSI.
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