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Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.

Abstract：

:A series of pyridine-linked indanone derivatives were designed and synthesized to discover new small molecules for the treatment of inflammatory bowel disease (IBD). Compounds 5b and 5d exhibited strongest inhibitory activity against TNF-α-induced monocyte adhesion to colon epithelial cells (an in vitro model of colitis). In TNBS (2,4,6-trinitrobenzenesulfonic acid)-induced rat colitis model, oral administration of the compounds 5b and 5d ameliorated colitis with significant recovery in altered expressions of E-cadherin, TNF-α and IL-1β expressions, indicating 5b and 5d as potential agents for therapeutics development against IBD.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kadayat TM,Banskota S,Bist G,Gurung P,Magar TBT,Shrestha A,Kim JA,Lee ES

doi

10.1016/j.bmcl.2018.06.012

subject

Has Abstract

pub_date

2018-08-01 00:00:00

pages

2436-2441

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30500-6

journal_volume

28

pub_type

杂志文章

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