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Synthesis and anti-inflammatory evaluation of N-sulfonyl anthranilic acids via Ir(III)-catalyzed C-H amidation of benzoic acids.

Abstract：

:The iridium(III)-catalyzed ortho-C-H amidation of benzoic acids with sulfonyl azides is described. These transformations allow the facile generation of N-sulfonyl anthranilic acids, which are known as crucial scaffolds found in biologically active molecules. In addition, all synthetic products were evaluated for in vitro anti-inflammatory activity against interleukin-1β (IL-1β) and cyclooxygenase-2 (COX-2) with lipopolysaccharide (LPS)-induced RAW264.7 cells. Notably, compounds 4c and 4d, generated from p-OMe- and p-Br-sulfonyl azides, were found to display potent anti-inflammatory property stronger than that of well-known NSAIDs ibuprofen.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Han SH,Suh HS,Jo H,Oh Y,Mishra NK,Han S,Kim HS,Jung YH,Lee BM,Kim IS

doi

10.1016/j.bmcl.2017.03.072

subject

Has Abstract

pub_date

2017-05-15 00:00:00

pages

2129-2134

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30322-0

journal_volume

27

pub_type

杂志文章

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