Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biozentrum, ZAFES/LiFF/CMP/ICNF, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5883-6. doi: 10.1016/j.bmcl.2010.07.109. Epub 2010 Aug 1.
With a small series of compounds we demonstrated the variability in the core region of the human histamine H(3) receptor (hH(3)R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Additional variations achieved by coupling different residues to the heterocyclic core structure led to further optimisation of in vitro receptor binding of the novel azole derivatives.
通过引入极性唑基团(恶唑、噁二唑、噻唑和三唑),我们用一小系列化合物展示了人类组胺 H(3)受体(hH(3)R)拮抗剂结构蓝图核心区域的可变性。通过将不同的残基与杂环核心结构偶联实现的其他变化导致新型唑衍生物的体外受体结合进一步优化。