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Abstract <p><b>Objective:</b> Hyperuricemia is a major cause of gout. Over time, currently available drugs may become less effective. This study focuses on the synthesis and biological evaluation of new 3-chloro-1-phenyl-1<i>H</i>-pyrazolo[4,3-<i>c</i>]quinoline derivatives (<b>IIIa–IIIl</b>) as promising xanthine oxidase inhibitors for the treatment of gout. <b>Methods:</b> 3-chloro-1-phenyl-1<i>H</i>-pyrazolo[4,3-<i>c</i>]quinoline derivatives (<b>IIIa–IIIl</b>) were synthesized by reacting 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with various reagents. The structures of the synthesized compounds were established using various analytical techniques. The compounds were further evaluated for their in vitro xanthine oxidase inhibitory activity. <b>Results and Discussion:</b> Among the tested compounds, compound <b>IIIe</b> exhibited significant activity with an IC<sub>50</sub> value of 4.48 ± 0.12 µg/mL, compared to the standard drug allopurinol (9.45 ± 0.08 µg/mL). A docking study was performed to understand the molecular interactions of the leading compound. Compound <b>IIIe</b> showed a binding energy of –7.351 kcal/mol, which was more favorable than that of the standard (–5.387 kcal/mol). This indicates that the compounds are well docked into the active site of the protein. <b>Conclusions:</b> The 3-chloro-1-phenyl-1<i>H</i>-pyrazolo[4,3-<i>c</i>]quinoline derivatives (<b>IIIa–IIIl</b>) have demonstrated significant xanthine oxidase inhibitory properties. These findings suggest that these compounds could contribute to the development of new drugs for hyperuricemia and gout treatment.</p>

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Insight into New Quinoline-Pyrazole Hybrids as a Potential Xanthine Oxidase Inhibitor: Synthesis, Characterization, In Vitro and In Silico Studies

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • Pushpalatha Vodgalayya,
  • Ramith Ramu,
  • Deepthi Puttegowda,
  • Yeriyur Basavaiah Basavaraju

摘要

Abstract

Objective: Hyperuricemia is a major cause of gout. Over time, currently available drugs may become less effective. This study focuses on the synthesis and biological evaluation of new 3-chloro-1-phenyl-1H-pyrazolo[4,3-c]quinoline derivatives (IIIa–IIIl) as promising xanthine oxidase inhibitors for the treatment of gout. Methods: 3-chloro-1-phenyl-1H-pyrazolo[4,3-c]quinoline derivatives (IIIa–IIIl) were synthesized by reacting 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with various reagents. The structures of the synthesized compounds were established using various analytical techniques. The compounds were further evaluated for their in vitro xanthine oxidase inhibitory activity. Results and Discussion: Among the tested compounds, compound IIIe exhibited significant activity with an IC50 value of 4.48 ± 0.12 µg/mL, compared to the standard drug allopurinol (9.45 ± 0.08 µg/mL). A docking study was performed to understand the molecular interactions of the leading compound. Compound IIIe showed a binding energy of –7.351 kcal/mol, which was more favorable than that of the standard (–5.387 kcal/mol). This indicates that the compounds are well docked into the active site of the protein. Conclusions: The 3-chloro-1-phenyl-1H-pyrazolo[4,3-c]quinoline derivatives (IIIa–IIIl) have demonstrated significant xanthine oxidase inhibitory properties. These findings suggest that these compounds could contribute to the development of new drugs for hyperuricemia and gout treatment.