Prodrugs of NSAIDs: A Review

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Prodrugs of NSAIDs: A Review

Intoroduction Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action. Methods & Materials The two different pharmacophores combine to give synergistic activity or may hel...

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The design and the synthesis of prodrugs for nonsteroidal anti-inflammatory drugs (NSAIDs) have been given much attention by medicinal chemists, especially in the last decade. As a therapeutic group, NSAIDs are among the most widely used prescribed and over the counter (OTC) medications. The rich literature about potential NSAID prodrugs clearly shows a shift from alkyl, aryalkyl or aryl esters...

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Amide prodrugs of NSAIDs: Synthesis and biological evaluation with a hydrolysis study

The aim of the present study was to synthesize prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation and bleeding) associated with their use. A total of six amide-based prodrugs (Ia-f) of aceclofenac, diclofenac, fenbufen, indomethacin, mefenamic acid and 4-biphenyl acetic acid were synthesized through one-pot method (single step synthesis). The structures of th...

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ژورنال

عنوان ژورنال: The Open Medicinal Chemistry Journal

سال: 2017

ISSN: 1874-1045

DOI: 10.2174/1874104501711010146