对抗
化学
喹唑啉
药物发现
药理学
立体化学
敌手
结构-活动关系
鉴定(生物学)
组合化学
受体
体外
生物化学
医学
植物
生物
作者
Gábor Szántó,Attila Makó,István Vágó,Tamás Hergert,Imre Bata,Bence Farkas,Sándor Kolok,Mónika Vastag
标识
DOI:10.1016/j.bmcl.2016.07.013
摘要
Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds 51 is presented.
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