2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists

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• 作者：Miriam André ; s ; Mó ; nica Bravo ; Maria Antonia Buil ; Marta Calbet ; Jordi Castro ; Teresa Domè ; nech ; Peter Eichhorn ; Manel Ferrer ; Elena Gó ; mez ; Martin D. Lehner ; Imma Moreno ; Richard S. Roberts ; ^{rick.roberts@almirall.com} ; Sara Sevilla
• 关键词：CRTh2 ; Prostaglandin D2 ; Antagonist ; Pyrazole ; Plasma protein binding
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 June, 2013
• 年：2013
• 卷：23
• 期：11
• 页码：3349-3353
• 全文大小：1169 K

文摘

High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR but also identified some low nanomolar inhibitors.