The synthesis and the antioxidant activity of 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2a,4a,8a-triazacyclopenta[cd]azulene-3-carboxylic (or carbothionic) acid derivatives
New 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[ cd ]azulene-3-carboxylic (or carbothionic) acid derivatives have been designed, synthesized and evaluated for their in vitro antioxidant activity under conditions of the artificial oxidative stress using ionol, ascorbic acid an...
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Veröffentlicht in: | Farmacija 2021-02, Vol.68 (1), p.251-258 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
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Zusammenfassung: | New 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[
cd
]azulene-3-carboxylic (or carbothionic) acid derivatives have been designed, synthesized and evaluated for their
in vitro
antioxidant activity under conditions of the artificial oxidative stress using ionol, ascorbic acid and α-tocopherol as the reference drugs. It has been found that 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[
cd
]azulene-3-carbothionic acid derivatives
9b, 9c, 9d, 9e, 9f, 9i
and 1-phenoxymethyl-4-(4
1
-chlorophenyl)-5,6,7,8-tetrahydro-2,2a,8-triazacyclopenta[
cd
]azulene-3-carboxylic acid phenylamide
10
reveal a high antioxidant activity and a good
in silico
pharmacokinetic profile. The data obtained allowed us to select the most promising objects from the substances synthesized for further pharmacological screening for the presence of the antioxidant activity
in vivo
. |
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ISSN: | 0428-0296 2603-557X |
DOI: | 10.3897/pharmacia.68.e60195 |