Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity.
The synthesis and pharmacological evaluation of a series of amide derivatives of NSAIDs with L-cysteine ethyl ester is described. The novel derivatives are potent antiinflammatory, antioxidant and hypocholesterolemic-hypolipidemic agents, while they demonstrate considerably reduced gastrointestinal toxicity. This molecular modification may offer a general route to safer antiinflammatory agents, potentially suitable for chronic use in conditions such as neurodegenerative disorders.
Galanakis
Dimitrios
D
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 541 24 Thessaloniki, Greece. dgalana@pharm.auth.gr
Kourounakis
Angeliki P
AP
Tsiakitzis
Karyophyllis C
KC
Doulgkeris
Christos
C
Rekka
Eleni A
EA
Gavalas
Antonios
A
Kravaritou
Constantina
C
Charitos
Christos
C
Kourounakis
Panos N
PN
D000577:Amides / Q000009:adverse effects / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000138:chemical synthesis / Q000494:pharmacology*; D000975:Antioxidants / Q000009:adverse effects / Q000138:chemical synthesis / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood / Q000378:metabolism; D003545:Cysteine / Q000031:analogs & derivatives* / Q000737:chemistry*; D004341:Drug Evaluation; D005767:Gastrointestinal Diseases / Q000139:chemically induced*; D008077:Lipoproteins, LDL / Q000097:blood / Q000378:metabolism; D051379:Mice; D051381:Rats; D014280:Triglycerides / Q000097:blood / Q000378:metabolism
D000577:Amides; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D008077:Lipoproteins, LDL; D014280:Triglycerides; C031752:ethyl cysteine; D002784:Cholesterol; D003545:Cysteine