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2004
Amino acids
U 0400
Synthesis and Pharmacological Evaluation of Amide Conjugates of NSAIDs with
Ethyl Ester, Combining Potent Antiinflammatory and Antioxidant
47- 168 L-Cysteine
Properties with Significantly Reduced Gastrointestinal Toxicity. — Preliminary
results on the design, synthesis and pharmacological evaluation of seven amide derivatives of well established nonsteroidal antiinflammatory drugs (NSAIDs) with
L-cysteine ethyl ester are presented. Compounds (I) are prepared by direct amidation
of the carboxylic group of the respective NSAIDs. The novel compounds are potent
antiinflammatory, antioxidant and hypocholesterolemic-hypolipidemic agents with
essentially reduced gastrointestinal toxicity. Using this way of derivatization, safer antiinflammatory agents possessing additional, beneficial properties such as antiatheromatic activity may be obtained, which are candidates for long term administration in
neurodegenerative diseases. — (GALANAKIS*, D.; KOUROUNAKIS, A. P.;
TSIAKITZIS, K. C.; DOULGKERIS, C.; REKKA, E. A.; GAVALAS, A.;
KRAVARITOU, C.; CHARITOS, C.; KOUROUNAKIS, P. N.; Bioorg. Med. Chem.
Lett. 14 (2004) 14, 3639-3643; Dep. Pharm. Chem., Sch. Pharm., Aristotle Univ.,
GR-54006 Thessaloniki, Greece; Eng.) — H. Hoennerscheid
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