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Bioorg Med Chem Lett. 2011 Nov 1;21(21):6577-81. doi: 10.1016/j.bmcl.2011.08.014. Epub 2011 Aug 19.

Tricyclic aminopyrimidine histamine H4 receptor antagonists.

Author information

1
Johnson & Johnson Pharmaceutical Research & Development, LLC 3210 Merryfield Row, San Diego, CA 92121, USA. bsavall@its.jnj.com

Abstract

This report discloses the development of a series of tricyclic histamine H(4) receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H(4) receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.

PMID:
21920744
DOI:
10.1016/j.bmcl.2011.08.014
[Indexed for MEDLINE]

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