Synthesis and antioxidant activity study of pyrazoline carrying arylfuran/thiophene moiety

Abstract

A novel series of N-acetyl-3-aryl-5-(5-(p/o-nitrophenyl)-2-furyl/ /thienyl)-substituted pyrazolines (3a-o) were synthesized by the reaction of 1-aryl-3-(5-(p/o-nitrophenyl)-2-furyl/thienyl)-2-propene-1-ones with hydrazine hydrate in acetic acid medium. The structures of the newly synthesized compounds were established by IR, 1 H-NMR, mass spectra and a single-crystal X-ray study. The antioxidant activities of the synthesized compounds were determined using the DPPH scavenging assay. The compounds 3a, 3f, 3h and 3o showed moderate activity.

Combretastatin analogues in cancer biology: A prospective view

“…The nitrogen-containing heterocyclic pyrazole and pyrozole containing derivatives have been attributed with the ability to exert important antiangiogenic, antioxidant and anticancer action. 54,66,67 One has to add a rider here that these findings are from in vitro assays.…”

“…The combretastatin derivatives with benzofuran or benzothiophene replacement of the B ring were highly cytotoxic. 26,27,54,55 Thiophene and benzo[b]thiophene modified combretastatin and isocombretastatin bearing a 1,1-diarylethylene scaffold have been tested for bioactivity, 56 but the outcome does not appear to be of much significance. However, that had been reported earlier to be metabolised to an active form.…”

Pyrazoline as a medicinal scaffold

“…Pyrazole exhibits various biological activities and also has a potent medicinal scaffold 5 . Pyrazoline and its derivatives are having an antibacterial 6 , antimicrobial 7 , anti-inflammatory 8 , antioxidant 9 , antidiabetic 10 , anticancer 11 , antifungal 12 , antidepressant 13 , anticonvulsant 14 , analgesic 15 , and monoamine oxidases (MAOs) 16 .…”

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“…Among the five-membered heterocyclic templets,nitrogen and sulfur-containing heterocycles such as pyrazole, thiophene, pyrazoline, thiazole, and thiazolone have shown a broad spectrum of biological activities like anticancer, 5 antidiabetics, 6 antimicrobial, [7][8] tubercular, 9 antioxidant, 10 antiinflammatory 11 etc. Among these, thiazole and thiazolone are building blocks for several natural products as they are mainly found in Vitamin B 1 (thiamine).…”