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Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor
Masakazu Fujita1, Taketsugu Seki, Haruaki Inada
1Omiya Research Laboratory, Nikken Chemicals Co., Ltd., 1-346, Kitabukuro-cho, Saitama-shi, 330-0835, Saitama, Japan. souyaku@jade.dti.ne.jp
Bioorganic & Medicinal Chemistry Letters
|February 23, 2002
Abstract:
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]triazolo[4,3-a]diazepine (12) is excellent orally dual-acting PAF antagonist/TxSI.