Inhibitory activities of bipyrazoles: a patent review

Bipyrazole is constituted from two pyrazole units either in their fully aromatic or partially hydrogenated forms. Pyrazoles are widely available in pharmaceutical and agrochemical products. Some pyrazoles are essential parts of commercial drugs in the market. This inspired us to collect the pharmacological activities of bipyrazoles that have potential therapeutic behaviors in several biological aspects but none of them were included in commercial drugs.

This review covers all biological and pharmacological potentials of bipyrazole derivatives during 2010-2021. The topics of this review comprised anticancer, antioxidant, anti-inflammatory, antimicrobial, antitubercular, antimalarial, insecticidal activities as well as enzymatic inhibitions.

Bipyrazoles demonstrated a wide array of potent activities against various diseases such as anticancer, antitubercular, anti-inflammatory, and antimicrobial activities. Those are of great benefits for medicinal researchers to develop promising building blocks of bipyrazoles for treatment of diseases. The SAR studies showed that metallated bipyrazoles had better biological activities than bipyrazole ligands. For example, gold(III) and iridium(II) complexes of bipyrazoles were proved to be anticancer agents, and copper(I) as well as silver(I) complexes had excellent antibacterial activities. Several bipyrazoles were reported as antimalarial inhibitors better than chloroquine, the possible COVID-19 drug.