Abstract
We have designed and synthesized a series of novel molecules having a residue of a classical NSAID and an antioxidant moiety, both attached through amide bonds to a known nootropic structure, an L-proline, trans-4-hydroxy-L-proline or DL-pipecolinic acid residue. The compounds were found to retain anti-inflammatory and antioxidant activities, to acquire hypocholesterolemic action, and to possess a greatly reduced gastrointestinal toxicity. The novel molecules could find useful applications, among others, in slowing the progression or delaying the onset of neurodegenerative diseases.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Anticholesteremic Agents / chemical synthesis
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Anticholesteremic Agents / chemistry
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Anticholesteremic Agents / pharmacology
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / pharmacology*
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Arthritis / drug therapy*
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Cholesterol / blood
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Disease Models, Animal
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Drug Design
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Drug Evaluation, Preclinical
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Female
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Inflammation / drug therapy*
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Pipecolic Acids / chemical synthesis
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Pipecolic Acids / chemistry
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Pipecolic Acids / pharmacology*
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Proline / analogs & derivatives
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Proline / chemical synthesis
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Proline / pharmacology*
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Rats
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Rats, Inbred F344
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Structure-Activity Relationship
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Triglycerides / blood
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Anticholesteremic Agents
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Antioxidants
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Pipecolic Acids
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Triglycerides
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Cholesterol
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Proline