| Literature DB >> 25466180 |
Machhindra Gund1, Parikshit Gaikwad2, Namdev Borhade1, Aslam Burhan2, Dattatraya C Desai3, Ankur Sharma2, Mini Dhiman3, Mohan Patil2, Javed Sheikh1, Gajanan Thakre1, Santhosh G Tipparam1, Somesh Sharma2, Kumar V S Nemmani2, Apparao Satyam4.
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.Entities:
Keywords: Gastric-sparing NSAIDs; NO-NSAIDs; NO-aspirin; NO-naproxen; Nitric oxide donors
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Year: 2014 PMID： 25466180 DOI： 10.1016/j.bmcl.2014.10.096
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823