核医学与放射治疗

A Concise Review on the Synthesis of Pyrazole Heterocycles

Abstract

Ayaz Mahmood Dar and Shamsuzzaman

Study background: Pyrazole moiety, being called as pharmacophore, plays an important role in many biologically active compounds and therefore represents an interesting template for combinatorial as well as medicinal chemistry. In addition pyrazoles are also used extensively as useful synthons in organic synthesis. These derivatives have wide spread biological activities such as anticancer, analgesic, anti-inflammatory, antimicrobial, antiviral, anticonvulsant, antihistaminic and anti-HIV. The recent success of pyrazole COX-2 inhibitor has further highlighted the importance of these heterocycles in medicinal chemistry.

Methodology: The steps included condensation followed by cyclization or MCR, either in a step-wise manner or in one pot has been achieved successfully to obtain this class of heterocycles under different conditions. Phosphorus oxychloride (POCl3 ), dimethyl formamide, acetamide and hydrazine are the most common reagents used for the synthesis of pyrazole appended heterocyclic skeletons. Results: The reaction schemes resulted in the synthesis of heterocyclic appended pyrazoles in potential yields under either simple reaction conditions or microwave irradiation.

Conclusion: These protocols provide convenient strategies to annelate different heterocyclic nuclei with widespread bioactive pyrazoles thereby extending the categories of heterocyclic systems. These strategies also provide valuable information for the further design of more active biological agents through various modifications and derivatizations.