Pyrazole: an emerging privileged scaffold in drug discovery.

Future Med Chem

Department of Chemistry & Physics, College of Sciences & Mathematics, Arkansas State University Jonesboro, Jonesboro, AR 72467, USA.

Published: November 2023

AI Article Synopsis

  • Pyrazole, a five-membered chemical compound, is featured in many approved drugs and natural products, with numerous derivatives explored for treating various diseases.
  • Over the past decade, the number of drugs containing a pyrazole structure has surged, including well-known medications like ibrutinib, ruxolitinib, and sildenafil for conditions like cancer and erectile dysfunction.
  • Recent studies have also identified aniline-derived pyrazole compounds as effective antibacterial agents against resistant strains of bacteria.

Article Abstract

Pyrazole or 1-pyrazole, a five-membered 1,2-diazole, is found in several approved drugs and some bioactive natural products. A myriad number of derivatives of this small molecule have been reported in clinical and preclinical studies for the potential treatment of several diseases. The number of drugs containing a pyrazole nucleus has increased significantly in the last 10 years. Some of the best-selling drugs in this class are ibrutinib, ruxolitinib, axitinib, niraparib and baricitinib, and are used to treat different types of cancers; lenacapavir to treat HIV; riociguat to treat pulmonary hypertension; and sildenafil to treat erectile dysfunction. Several aniline-derived pyrazole compounds have been reported as potent antibacterial agents with selective activity against methicillin-resistant and vancomycin-resistant enterococci. Here, we discuss the pyrazole-derived drugs reported up to September 2023.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10652296PMC
http://dx.doi.org/10.4155/fmc-2023-0207DOI Listing

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