title: 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.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 541 24 Thessaloniki, Greece. dgalana@pharm.auth.gr
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Galanakis
authors.forename: Angeliki P
authors.initials: AP
authors.lastname: Kourounakis
authors.forename: Karyophyllis C
authors.initials: KC
authors.lastname: Tsiakitzis
authors.forename: Christos
authors.initials: C
authors.lastname: Doulgkeris
authors.forename: Eleni A
authors.initials: EA
authors.lastname: Rekka
authors.forename: Antonios
authors.initials: A
authors.lastname: Gavalas
authors.forename: Constantina
authors.initials: C
authors.lastname: Kravaritou
authors.forename: Christos
authors.initials: C
authors.lastname: Charitos
authors.forename: Panos N
authors.initials: PN
authors.lastname: Kourounakis
mesh_terms: 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
chemical_list: D000577:Amides; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D008077:Lipoproteins, LDL; D014280:Triglycerides; C031752:ethyl cysteine; D002784:Cholesterol; D003545:Cysteine