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Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.

Abstract：

:The optimization of a series of 4-(dimethylamino)quinazoline antagonists of the melanin-concentrating hormone receptor 1 (MCH-R1) is described. The combination of the elaboration of both the linker portion and the terminal phenyl ring provided N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-3,4-difluorobenzamide hydrochloride 28 (ATC0175), which showed excellent antagonist activity at the MCH-R1 (IC50 = 3.4 nM) as well as good selectivity over the Y5 and the alpha2A receptors.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kanuma K,Omodera K,Nishiguchi M,Funakoshi T,Chaki S,Semple G,Tran TA,Kramer B,Hsu D,Casper M,Thomsen B,Sekiguchi Y

doi

10.1016/j.bmcl.2005.05.121

subject

Has Abstract

pub_date

2005-09-01 00:00:00

pages

3853-6

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00713-4

journal_volume

15

pub_type

杂志文章

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