MUMBAI, India, April 17 -- Intellectual Property India has published a patent application (202621021135 A) filed by Vishwakarma Diksha; Vengurlekar Sudha; and Jain Sachin, Indore, Madhya Pradesh, on Feb. 23, for 'novel benzimidazole derivatives as cyclooxygenase inhibitors and a process for their synthesis.'
Inventor(s) include Vishwakarma Diksha; Vengurlekar Sudha; and Jain Sachin.
The application for the patent was published on April 17, under issue no. 16/2026.
According to the abstract released by the Intellectual Property India: "The present invention relates to novel benzimidazole derivatives and a process for their synthesis, characterization, and application as anti-inflammatory agents. The disclosed compounds are designed to inhibit cyclooxygenase enzymes (COX-1 and COX-2), which play a key role in prostaglandin-mediated inflammatory responses. The invention further addresses limitations associated with conventional non-steroidal anti-inflammatory drugs by providing compounds with improved binding affinity and favorable pharmacokinetic properties. In accordance with the invention, a series of substituted benzimidazole derivatives were rationally designed using structure-based molecular docking against COX-1 and COX-2 enzymes. The compounds were synthesized through a multistep chemical process involving condensation, acylation, and base-catalyzed reactions to yield chalcone-linked benzimidazole derivatives. The synthesized compounds were characterized using physicochemical and spectroscopic techniques including melting point determination, thin layer chromatography, elemental analysis, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectrometry. In-vitro anti-inflammatory activity of the synthesized derivatives was evaluated using cyclooxygenase inhibition assays, wherein selected compounds exhibited significant and dose-dependent inhibition of COX enzymes comparable to standard anti-inflammatory drugs. Additionally, in-silico ADME analysis indicated favorable drug-likeness and pharmacokinetic profiles suitable for oral administration. The invention thus provides novel benzimidazole-based compounds, a reproducible method of preparation, and their use as potential anti-inflammatory agents, making them suitable for pharmaceutical development in the treatment of inflammatory disorders. Keywords: Benzimidazole derivatives; Anti-inflammatory agents; Cyclooxygenase inhibition; COX-1 and COX-2; Molecular docking; Structure-based drug design; Chalcone-linked benzimidazoles; In-vitro COX inhibition assay; SwissADME analysis; Pharmaceutical compositions; Drug-likeness; Medicinal chemistry."
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