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Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists.

Abstract：

:We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stability when incubated in human and rat microsomes.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu S,Liu Y,Wang H,Ding Y,Wu H,Dong J,Wong A,Chen SH,Li G,Chan M,Sawyer N,Gervais FG,Henault M,Kargman S,Bedard LL,Han Y,Friesen R,Lobell RB,Stout DM

doi

10.1016/j.bmcl.2009.08.014

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

5741-5

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01129-9

journal_volume

19

pub_type

杂志文章

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