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Gastric-sparing nitric oxide-releasable 'true' prodrugs of aspirin and naproxen.

Abstract：

:Nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) are gaining attention as potentially gastric-sparing NSAIDs. Herein, we report a novel class of '1-(nitrooxy)ethyl ester' group-containing NSAIDS as efficient NO releasing 'true' prodrugs of aspirin and naproxen. While an aspirin prodrug exhibited comparable oral bioavailability and antiplatelet activity (i.e., TXB2 inhibition) to those of aspirin, a naproxen prodrug exhibited better bioavailability than naproxen. These promising NO-NSAIDs protected experimental rats from gastric damage. We therefore believe that these promising NO-NSAIDs could represent a new class of potentially 'Safe NSAIDs' for the treatment of arthritic pain, inflammation and cardiovascular disorders in the case of NO-aspirin.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gund M,Gaikwad P,Borhade N,Burhan A,Desai DC,Sharma A,Dhiman M,Patil M,Sheikh J,Thakre G,Tipparam SG,Sharma S,Nemmani KVS,Satyam A

doi

10.1016/j.bmcl.2014.10.096

subject

Has Abstract

pub_date

2014-12-15 00:00:00

pages

5587-5592

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01167-6

journal_volume

24

pub_type

杂志文章

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