Design,Synthesis and Biological Evaluation of Novel Derivatives of Laropiprantas Potent Prostaglandi

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户:kenlixin
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  Laropiprant,approved by the European Medicines Agency(EMA) in 2008,is used in combination with nicotinic acid to reduce blood cholesterol.Laropiprant itself,as a prostaglandin D2 receptor 1(DP1) antagonist,has no cholesterol lowering effect,but it can reduce facial flushes induced by nicotinic acid.The SAR about the analogue of laropiprant showed that the indole scaffold,N-benzyl substituent and a carboxylic acid moiety is important for antagonizing DP1.
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