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<p>Novel nicotinic acid derivatives were synthesized as potent anti-diabetic agents. The developed inhibitors were investigated for their pharmacological in vitro screening, such as anti-diabetic, anti-inflammation, and in silico analysis. It has good interactions with α-amylase protein, with a range of -7.18 to -5.55&#xa0;kcal/mol. The inhibitors were synthesized by employing the Steglich-type reaction to couple alcohol and amine derivatives. These molecules were characterized using NMR, FT-IR, and Mass spectrometry techniques. Anti-hyperglycemic activity has been screened using α-amylase protein, and the half-maximal inhibition efficiency (IC<sub>50</sub>) value was evaluated, ranging from 1.324 ± 0.17 to 1.516 ± 0.14&#xa0;µg. The positive control (acarbose) range is 1.273 ± 0.12&#xa0;µg. Induced human RBC hemolysis assay was utilized for anti-inflammatory activity, and the cumulative observation results were compared with the reference drug (ketorolac- IC<sub>50</sub> = 11.79 ± 0.17 µM), with IC<sub>50</sub> values between 14.06 ± 0.15 to 85.56 ± 0.25 µM. Moreover, the antioxidant ability of synthesized inhibitor compounds was evaluated by radical scavenging methods. The efficacy of inhibitors <b>2b</b> and <b>2&#xa0;h</b> (IC<sub>50</sub> = 15.63 ± 0.13 µM and 12.88 ± 0.19 µM (DPPH), IC<sub>50</sub> = 19.89 ± 0.25 µM and 16.35 ± 0.25 µM (ABTS)) exhibited good results against DPPH and ABTS radicals with ascorbic acid(standard) (DPPH: IC<sub>50</sub> = 11.81 ± 0.04 µM and ABTS: 11.90 ± 0.01 µM). The synthesized derivatives show promising results of anti-inflammatory and anti-hyperglycemic properties. This provides a path to developing the new therapeutic agents for inflammation.</p>

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Discovery of new pyridine 3-carboxylic acid-based pharmacophores as dual anti-inflammatory and anti-hyperglycemic agents

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年10月3日

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  • K. Ramakrishnan,
  • Lenin Nachimuthu,
  • Reshma Rajan,
  • J. Premkumar,
  • Vallabh Mulay,
  • S. Meenakshi,
  • Chandrakala A. Narasimhulu,
  • Pragney Deme,
  • Sanjay Rajagopalan,
  • Ramanathan Lalgudi,
  • Akella Sivaramakrishna,
  • S. Karthikeyan,
  • Rajagopal Desikan

摘要

Novel nicotinic acid derivatives were synthesized as potent anti-diabetic agents. The developed inhibitors were investigated for their pharmacological in vitro screening, such as anti-diabetic, anti-inflammation, and in silico analysis. It has good interactions with α-amylase protein, with a range of -7.18 to -5.55 kcal/mol. The inhibitors were synthesized by employing the Steglich-type reaction to couple alcohol and amine derivatives. These molecules were characterized using NMR, FT-IR, and Mass spectrometry techniques. Anti-hyperglycemic activity has been screened using α-amylase protein, and the half-maximal inhibition efficiency (IC50) value was evaluated, ranging from 1.324 ± 0.17 to 1.516 ± 0.14 µg. The positive control (acarbose) range is 1.273 ± 0.12 µg. Induced human RBC hemolysis assay was utilized for anti-inflammatory activity, and the cumulative observation results were compared with the reference drug (ketorolac- IC50 = 11.79 ± 0.17 µM), with IC50 values between 14.06 ± 0.15 to 85.56 ± 0.25 µM. Moreover, the antioxidant ability of synthesized inhibitor compounds was evaluated by radical scavenging methods. The efficacy of inhibitors 2b and 2 h (IC50 = 15.63 ± 0.13 µM and 12.88 ± 0.19 µM (DPPH), IC50 = 19.89 ± 0.25 µM and 16.35 ± 0.25 µM (ABTS)) exhibited good results against DPPH and ABTS radicals with ascorbic acid(standard) (DPPH: IC50 = 11.81 ± 0.04 µM and ABTS: 11.90 ± 0.01 µM). The synthesized derivatives show promising results of anti-inflammatory and anti-hyperglycemic properties. This provides a path to developing the new therapeutic agents for inflammation.