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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 .

pharmacia

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