Photochemistry Department (Heterocyclic Unit), National Research Center, 12622 Dokki, Giza, Egypt.
Acta Pharm. 2010 Sep;60(3):311-23. doi: 10.2478/v10007-010-0027-6.
2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3a), 1-(5-amino-4-(4-chloro-3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3b), 1-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl)pyrazolidine-3,5-dione (4), (Z)-N'-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) formohydrazonic acid (5a), (Z)-ethyl-N'-4-methyl-2-amino-5-acetylthiophene-3-carbonylformo hydrazonate (5b), 6-acetyl-3-amino-2,5-dimethylthieno[2,3-d]pyrimidin-4(3H)-one (8), 5-methyl-3-amino-2-mercapto-6-acetylthieno [2,3-d]pyrimidin-4(3H)-one (10) and 5-methyl-6-acetyl-2-thioxo-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-one (12) as potential antioxidant and antitumor agents. Pharmacological tests showed that compounds 6a, 6b, 8, 10 and 12 exhibited significant antitumor and antioxidant activity.
2-氨基-5-乙酰基-4-甲基噻吩-3-羧酸乙酯（1）和 5-乙酰基-2-氨基-4-甲基噻吩-3-甲酰肼（2）被合成，并用作合成一系列新的 1-（5-氨基-4-（3,5-二甲基-1H-吡唑-1-羰基）-3-甲基噻吩-2-基）乙酮（3a）、1-（5-氨基-4-（4-氯-3,5-二甲基-1H-吡唑-1-羰基）-3-甲基噻吩-2-基）乙酮（3b）、1-（4-甲基-2-氨基-5-乙酰基噻吩-3-甲酰基）吡唑烷-3,5-二酮（4）、（Z）-N' -（4-甲基-2-氨基-5-乙酰基噻吩-3-甲酰基）甲脒（5a）、（Z）-乙基-N'-4-甲基-2-氨基-5-乙酰基噻吩-3-甲酰基甲脒（5b）、6-乙酰基-3-氨基-2,5-二甲基噻吩并[2,3-d]嘧啶-4(3H)-酮（8）、5-甲基-3-氨基-2-巯基-6-乙酰基噻吩并[2,3-d]嘧啶-4(3H)-酮（10）和 5-甲基-6-乙酰基-2-硫代-2,3-二氢噻吩并[2,3-d]嘧啶-4(1H)-酮（12）作为潜在的抗氧化和抗肿瘤药物。药理试验表明，化合物 6a、6b、8、10 和 12 表现出显著的抗肿瘤和抗氧化活性。
