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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 evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.

Author information

1
Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France. Electronic address: o.labeeuw@bioprojet.com.
2
Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France.

Abstract

Synthesis and biological evaluation of a new class of histamine H4 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.

KEYWORDS:

Asthma; Atopic dermatitis; Histamine; Histamine H(4) receptor

PMID:
27692832
DOI:
10.1016/j.bmcl.2016.09.049
[Indexed for MEDLINE]

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