首批强效且具选择性的非咪唑类人组胺H4受体拮抗剂。
The first potent and selective non-imidazole human histamine H4 receptor antagonists.
作者信息
Jablonowski Jill A, Grice Cheryl A, Chai Wenying, Dvorak Curt A, Venable Jennifer D, Kwok Annette K, Ly Kiev S, Wei Jianmei, Baker Sherry M, Desai Pragnya J, Jiang Wen, Wilson Sandy J, Thurmond Robin L, Karlsson Lars, Edwards James P, Lovenberg Timothy W, Carruthers Nicholas I
机构信息
Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, USA.
出版信息
J Med Chem. 2003 Sep 11;46(19):3957-60. doi: 10.1021/jm0341047.
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
在发现人类组胺H4受体之后，对我们公司化合物库进行的高通量筛选确定化合物6为潜在先导化合物。对构效关系的研究导致发现了新型化合物10e和10l，它们是首批被描述的强效且选择性的组胺H4受体拮抗剂。
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