Gastric-sparing nitric oxide-releasable 'true' prodrugs of aspirin and naproxen
| Autor: | Javed Sheikh, Aslam Burhan, Parikshit Gaikwad, Mohan Patil, Santhosh Goud Tipparam, Mini Dhiman, Machhindra Gund, Dattatraya C. Desai, Gajanan Thakre, Ankur Sharma, Namdev Borhade, Somesh Sharma, Apparao Satyam, Kumar V.S. Nemmani |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
musculoskeletal diseases
Blood Platelets Naproxen Clinical Biochemistry Pharmaceutical Science Inflammation Pharmacology Nitric Oxide digestive system Biochemistry Nitric oxide Rats Sprague-Dawley chemistry.chemical_compound Drug Stability Drug Discovery medicine Animals Humans Prodrugs skin and connective tissue diseases Molecular Biology Aspirin Nitrates Chemistry Organic Chemistry Anti-Inflammatory Agents Non-Steroidal NO-aspirin Ethyl ester Prodrug digestive system diseases Bioavailability Rats Thromboxane B2 ROC Curve Cyclooxygenase 2 Gastric Mucosa Area Under Curve Drug Design Cyclooxygenase 1 Molecular Medicine medicine.symptom Platelet Aggregation Inhibitors medicine.drug Half-Life |
| Zdroj: | Bioorganicmedicinal chemistry letters. 24(24) |
| ISSN: | 1464-3405 |
| Popis: | 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., TXB 2 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. |
| Databáze: | OpenAIRE |
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