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Bioorg Med Chem Lett. 2008 Dec 1;18(23):6041-5. doi: 10.1016/j.bmcl.2008.10.034. Epub 2008 Oct 11.

Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.

Author information

1
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd., 3 Okubo, Tsukuba, Ibaraki 300-2611, Japan.

Abstract

Novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives were identified as potent human H(3) receptor inverse agonists. After systematic modification of lead 5a, the potent and selective analog 5r was identified. Elimination of hERG K(+) channel and human alpha(1A)-adrenoceptor activities is the main focus of the present study.

PMID:
18952421
DOI:
10.1016/j.bmcl.2008.10.034
[Indexed for MEDLINE]

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