Antioxidant Activity of Novel Indole Derivatives and Protection of the Myocardial Damage in Rabbits

Novel indole derivatives containing a triazole moiety (1a—d, 2a—c) were synthesized as lead compounds with interesting pharmacological profiles. Their antioxidant activity was investigated on in vitro non-enzymatic rat hepatic microsomal lipid peroxidation. All compounds showed significant effect in...

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Bibliographic Details
Published in:	Chemical & pharmaceutical bulletin Vol. 50; no. 2; pp. 165 - 168
Main Authors:	Andreadou, Ioanna, Tasouli, Androniki, Bofilis, Elias, Chrysselis, Michael, Rekka, Eleni, Tsantili-Kakoulidou, Anna, Iliodromitis, Efstathios, Siatra, Theodora, Kremastinos, Dimitrios Thoma
Format:	Journal Article
Language:	English
Published:	Tokyo The Pharmaceutical Society of Japan 01-02-2002 Maruzen Japan Science and Technology Agency
Subjects:	Animals antioxidant activity Antioxidants - pharmacology Biological and medical sciences Cardiovascular system indole derivative Indoles - pharmacology lipid peroxidation Lipid Peroxidation - drug effects Male malondialdehyde Malondialdehyde - analysis Medical sciences Miscellaneous myocardial infarction Myocardial Ischemia - drug therapy Myocardial Reperfusion Injury - prevention & control Pharmacology. Drug treatments Protective Agents - pharmacology Rabbits Rats Rats, Wistar Nitro compound Infarct Nitrogen heterocycle Rabbit Cardiovascular disease Lipids Myocardial disease Vascular disease Chlorine Organic compounds Bicyclic compound Aromatic compound Oxidation Chemical synthesis Peroxidation Cardioprotective agent Lagomorpha Antioxidant In vitro Biological activity In vivo Vertebrata Mammalia Animal Triazole derivatives Indole derivatives
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Summary:	Novel indole derivatives containing a triazole moiety (1a—d, 2a—c) were synthesized as lead compounds with interesting pharmacological profiles. Their antioxidant activity was investigated on in vitro non-enzymatic rat hepatic microsomal lipid peroxidation. All compounds showed significant effect in the above assay. The effect depended mainly on the attachment position of the triazole moiety on the indole nucleus. The most potent antioxidant derivatives 1a, 1c and 1d were tested for their protective ability against the oxidative damage of the myocardium after ischemia-reperfusion, in male rabbits which were subjected to 30 min regional ischemia followed by reperfusion. The tested antioxidant compounds 1a, 1c and 1d were continuously infused for 30 min starting at 10th min of ischemia and lasted at 10th min of reperfusion. The concentration of malondialdehyde (MDA, a marker of lipid peroxidation) and hemodynamic parameters (blood pressure and heart rate) were measured in the baseline, at 20th min of the sustained ischemia, 1st and 20th min of reperfusion. It was found that the examined compounds 1a, 1c and 1d reduced significantly the level of MDA in rabbits under ischemia-reperfusion and proved to be promising substances for further evaluation of anti-ischemic properties.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.50.165