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Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.

Abstract：

:A novel series of 4-pyridazin-3-one and 5-pyridazin-3-one analogues were designed and synthesized as H(3)R antagonists. Structure-activity relationship revealed the 5-pyridazin-3-ones 8a and S-methyl 8b had excellent human and rat H(3)R affinities, and acceptable pharmacokinetic properties. In vivo evaluation of 8a showed potent activity in the rat dipsogenia model and robust wake-promoting activity in the rat EEG/EMG model.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Becknell NC,Lyons JA,Aimone LD,Huang Z,Gruner JA,Raddatz R,Hudkins RL

doi

10.1016/j.bmc.2012.04.028

subject

Has Abstract

pub_date

2012-06-15 00:00:00

pages

3880-6

issue

12

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00312-4

journal_volume

20

pub_type

杂志文章

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