Keywords
Antioxidant
N-acetyl
Pyrazoline
Abstract
In medicinal chemistry, the pyrazoline structure was found to be an advantaged moiety due to its broad spectrum of pharmacological properties. The study aims on the synthesis, characterization, and in vitro antidiabetic and antioxidant activity evaluation of heteroaryl para chloro N-acetyl pyrazoline derivatives. The synthesis begins with the reaction of previously synthesized heteroaryl chalcone derivatives and hydrazine hydrate in presence of acetic acid using reflux method for 4hrs. The synthesized derivatives were purified using thin layer chromatography, obtained in a good yield and characterized using FT-IR, 1HNMR and 13CNMR spectroscopies. The in vitro antidiabetic was assessed using α-amylase inhibitory assay utilizing acarbose as reference standard. The result indicates that among the synthesized derivatives only compound 3b shows inhibition against α-amylase with IC50 value 90.49 ± 0.19 µM though higher compared to acarbose control standard with IC50 value 34.37 ± 0.14 µM and the result were statistically significant at (p < 0.05). Whereas the in vitro antioxidant activity was evaluated using DPPH assay employing ascorbic acid as reference standard. The result shows that all the synthesized heteroaryl para chloro N-acetyl pyrazoline derivatives gives negative or no radical scavenging activity due to the high lipophilic nature of the derivatives. In conclusion the heteroaryl para chloro N-acetyl pyrazoline derivatives were synthesized efficiently and the in vitro antidiabetic and antioxidant activities were assessed; it was found that only compound 3b inhibits α-amylase among the derivatives while none of the derivative show antioxidant activity. Other antidiabetic like α-glucoside and antioxidants like ABS are recommended for the synthesized derivatives in the preceding research.
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