A review on recent advances for the synthesis of bioactive pyrazolinone and pyrazolidinedione derivatives

Aly A Abd-Ella,Youssra A Naffea,Mokhtar A Abd Ul-Malik,Shaban A A Abdel-Raheem,Yasser A El-Ossaily,Saoud A Metwally,Fathy M Abd Elrazek,Safwat A Aref

doi:10.5267/j.ccl.2022.2.004

Aly A Abd-Ella, Youssra A Naffea + Show 6 more

Open Access

https://doi.org/10.5267/j.ccl.2022.2.004

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Abstract

Oxo derivatives of pyrazolines and pyrazolidines are important heterocyclic compounds due to their unique biological activities and have been widely applied in pharmaceutical and agromedical fields. In this review, we provide an account of some recent advances in the field of pyrazolone chemistry, specifically on the reported synthesis methods of pyrazolinone (3-oxo-1,2-dihydropyrazole) and 3,5-pyrzolidinediones (3,5-dioxotetrahydropyrazoles) derivatives.

Highlights

The heterocyclic compounds involving pyrazolinone (3-oxo-1,2-dihydropyrazole) and 3,5-pyrzolidinediones (3,5dioxotetrahydropyrazoles) were reported for their wide range of pharmacological and agricultural activities.1-5 The incorporation of an active scaffold in the structure of heterocyclic compounds enhances properties associated with them
We provide an account of some recent advances in the field of pyrazolone chemistry, on the reported synthesis methods of pyrazolinone (3-oxo1,2-dihydropyrazole) and 3,5-pyrzolidinediones (3,5-dioxotetrahydropyrazoles) derivatives
This review is concerned on the synthesis of bioactive pyrazolinone and pyrazolidinedione derivatives (Fig. 1)

Summary

Introduction

The heterocyclic compounds involving pyrazolinone (3-oxo-1,2-dihydropyrazole) and 3,5-pyrzolidinediones (3,5dioxotetrahydropyrazoles) were reported for their wide range of pharmacological and agricultural activities. The incorporation of an active scaffold in the structure of heterocyclic compounds enhances properties associated with them. The incorporation of an active scaffold in the structure of heterocyclic compounds enhances properties associated with them. This has proven useful in the development of newer effective heterocycles possessing several activities. This review is concerned on the synthesis of bioactive pyrazolinone and pyrazolidinedione derivatives (Fig. 1). The increasing importance of 3,5-pyrazolidinediones was due to their use as medical derivatives such as 4-butyl-1,2diphenyl-3,5-pyrazolidinedione [3] which was marked as butazolidin (phenylbutazone). It was widely used in the treatment of rheumatoid arthritis and various other diseases. Five isomeric forms of 3,5-pyrazolidinediones [1] are theoretically possible [4], [5], [6], [7] and [8] (Fig. 2)

H N N OH

Synthesis of 3,5-pyrazolidinedione derivatives

H N HN R

Synthesis of Pyrazolinone derivatives

Conclusion