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<p>Among the diversity of existing heterocycles, nitrogen-containing heterocycles, i.e., azaheterocycles, are the&#xa0;most popular entity in drug discovery. In the present review, we have focused on the structural diversity of pyrazole in drug discovery and the critical analysis of&#xa0;approved drugs bearing this versatile pharmacophore in the past decade (2014–2023). The investigation of the USFDA-approved drug-bearing pyrazole scaffold revealed that a total of 20 drugs were approved during the period of analysis. The bifurcation of approved drugs led us to conclude that nine drugs (45%) were to treat cancer, followed by four drugs for rare genetic diseases, three for treating infection, two for neurological conditions, and one for rheumatoid arthritis and glaucoma, respectively. The investigation also revealed that the majority of drugs (65%) were indicated to be used in rare forms of cancer and diseases. Besides this, the review also highlighted that 53% of approved drugs were launched in&#xa0;tablet form, and 80% of these drugs were intended to be given by oral route. The drug metabolism analysis revealed that 25% of approved drugs undergo Phase 1 metabolism via CYP3A4, followed by the combined involvement of CYP3A4 and CYP2C9 for 10% of approved drugs. The drugs are chiefly excreted via the&#xa0;fecal route (12) and the urine (7). The structural diversity revealed that the majority of pyrazole drugs comprised a pyridine ring (7) in conjugation. At the same time, fluorine was the key halogen substituent, and amine was the major non-halogenated substituent in the approved drugs. The review is, therefore, a congregated effort to not only compile and update the USFDA-approved drugs containing pyrazole but also explore their in-depth medicinal chemistry-based analysis to enrich the medicinal chemist and allied sciences researchers for their comprehensive read.</p> Graphical abstract <p></p>

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Pyrazole in drug development: a medicinal-chemistry based analysis of USFDA-approved drugs in last decade

  • 期刊论文

  • 发表日期：

    2025年6月23日

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  • Nisha Bansal,
  • Elagandhula Sathish,
  • M. Arockia Babu,
  • Ganesh Bushi,
  • Abhay M. Gaidhane,
  • Thakur Gurjeet Singh,
  • Damini Singh,
  • Glowi Alasiri,
  • Mohammad Fareed,
  • Bhupinder Kumar

摘要

Among the diversity of existing heterocycles, nitrogen-containing heterocycles, i.e., azaheterocycles, are the most popular entity in drug discovery. In the present review, we have focused on the structural diversity of pyrazole in drug discovery and the critical analysis of approved drugs bearing this versatile pharmacophore in the past decade (2014–2023). The investigation of the USFDA-approved drug-bearing pyrazole scaffold revealed that a total of 20 drugs were approved during the period of analysis. The bifurcation of approved drugs led us to conclude that nine drugs (45%) were to treat cancer, followed by four drugs for rare genetic diseases, three for treating infection, two for neurological conditions, and one for rheumatoid arthritis and glaucoma, respectively. The investigation also revealed that the majority of drugs (65%) were indicated to be used in rare forms of cancer and diseases. Besides this, the review also highlighted that 53% of approved drugs were launched in tablet form, and 80% of these drugs were intended to be given by oral route. The drug metabolism analysis revealed that 25% of approved drugs undergo Phase 1 metabolism via CYP3A4, followed by the combined involvement of CYP3A4 and CYP2C9 for 10% of approved drugs. The drugs are chiefly excreted via the fecal route (12) and the urine (7). The structural diversity revealed that the majority of pyrazole drugs comprised a pyridine ring (7) in conjugation. At the same time, fluorine was the key halogen substituent, and amine was the major non-halogenated substituent in the approved drugs. The review is, therefore, a congregated effort to not only compile and update the USFDA-approved drugs containing pyrazole but also explore their in-depth medicinal chemistry-based analysis to enrich the medicinal chemist and allied sciences researchers for their comprehensive read.

Graphical abstract