Metabolism study and biological evaluation of bosentan derivatives
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- 作者：Susan Lepri1 ; Laura Goracci1 ; Aurora Valeri ; Gabriele Cruciani ; gabriele.cruciani@unipg.it" class="auth_mail" title="E-mail the corresponding author
- 关键词：Bosentan ; Perfluorinated analogues ; Metabolic specificity ; Phase I metabolism ; HLM
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 October 2016
- 年：2016
- 卷：121
- 期：Complete
- 页码：658-670
- 全文大小：1275 K
文摘
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Bosentan derivatives were designed and synthesized to improve metabolic stability.
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Their metabolism in HLM, CYP3A4 and CYP2C9 was determined.
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Cytotoxicity and activity against endothelin receptors were studied.
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All compounds showed an improved metabolic stability towards CYP2C9.
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Compound 5c displayed a moderate antagonist effect towards ETA.