Synthesis of thiazole derivatives as cholinesterase inhibitors with antioxidant activity

Abstract

In the present research, we synthesized two unique series of thiazole compounds having 5-bromothiophene and 3-methylthiophene (2a-2f) in their structure. After that, spectroscopic methods were used to analyze the chemical compositions of the newly synthesized molecules. Then in vitro evaluation was done to determine acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activity of the synthesized compounds using galantamine as reference standard. The compounds’ antioxidant properties were assessed using DPPH radical scavenging and ferrous ion-chelating techniques. The results of the study showed weak anticholinesterase activity against AChE and BuChE enzymes for all the final compounds. The synthesized analogs also showed significant DPPH radical scavenging activities with IC50 values in the range of 29.16 ± 0.009 to 33.09 ± 0.004 µM (for DDPH) incomparison to standard gallic acid with IC50 = 31.13 ± 0.008 µM (for DDPH). Especially, compound 2c showed the best antioxidant activity with IC50 value of 29.16 ± 0.009 µM.

Keywords

• AChE
• Antioxidant
• BuChE
• Thiazole.

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