Labeeuw Olivier, Levoin Nicolas, Billot Xavier, Danvy Denis, Calmels Thierry, Krief Stéphane, Ligneau Xavier, Berrebi-Bertrand Isabelle, Robert Philippe, Lecomte Jeanne-Marie, Schwartz Jean-Charles, Capet Marc
Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France.
Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France.
Bioorg Med Chem Lett. 2016 Nov 1;26(21):5263-5266. doi: 10.1016/j.bmcl.2016.09.049. Epub 2016 Sep 19.
Synthesis and biological evaluation of a new class of histamine H receptor ligands, distinct from the previously reported chemotypes, are described. A virtual screening of our corporate compound collection identified a hit with an undesired dual H3R/H4R activity. Chemical exploration led to the discovery of a more potent and selective 2-benzothiazolylphenylmethyl ether lead compound.
本文描述了一类新型组胺H受体配体的合成及生物学评价，这类配体与先前报道的化学类型不同。对我们公司化合物库进行虚拟筛选，发现了一种具有不良H3R/H4R双重活性的命中化合物。通过化学探索，发现了一种更有效且更具选择性的2-苯并噻唑基苯基甲基醚先导化合物。
