Synthesis of 4-acyl- and 4-alkoxy-carbonylpyrazoles

Al-Saleh, Fowzia S.; Khawaja, Ibtisam K. Al; Joule, John A.

doi:10.1039/p19810000642

Cited by 8 publications

(1 citation statement)

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“…The compounds with pyrazole core are the most important class in active pharmaceutical drugs and remain the choice for anti-inflammatory agents in spite of multiple attempts at exploring alternative scaffolds. 9,10 Amongst the various methods available in the literature for the synthesis of pyrazole scaffolds, most commonly employed being; a base catalyzed reaction of hydrazines with 1,3-dicarbonyl compounds, 11 1,3-dipolar cycloaddition of hydrazones to alkenes, 12 and via Vilsmeier-Haack reaction of arylhydrazones. 13 Further, it is emphasized here that pyrazoles are regarded as promising molecules with potential applications in bioorganic chemistry.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of thiophene-pyrazole conjugates as potent antimicrobial and radical scavengers

Prabhudeva¹,

Renuka²,

Kumar³

2018

10.5267/j.ccl

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The current study presents the synthesis of thiophene-appended pyrazoles through 3+2 annulations of chalcones 3(a-g) with aryl hydrazine hydrochlorides 4(a-d) in acetic acid (30%) under reflux conditions produced the thiophene-pyrazole hybrids 5(a-g) in good yields. Structures of synthesized new pyrazoles were confirmed by spectral studies, and elemental analysis. Further, preliminary biological evaluation studies show that compounds 5b and 5f having chloro substitution only in the thiophene ring exhibited excellent inhibition (12.5-25.0 µg/mL) against all the tested organisms in comparison with that of the standard. Compounds, 5a, 5c and 5g having electronegative chloro substitutions each in the aromatic and thiophene rings showed excellent (12.423-31.213 µg mL -1 ) DPPH radical scavenging potencies. The synthesis of pyrazoline derivatives and the efficacy of some of the synthesized molecules as antimicrobial and antioxidant agents validate the significance of this study.

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