Intellectual Property India Publishes Patent Application for Novel 4-(hydrazinylphenyl)-6-(substituted Phenyl)pyrimidin-2(1h)-One Derivatives: Synthesis, Characterization, And Therapeutic Applications As Anticancer And Antibacterial Agents

MUMBAI, India, June 22 -- Intellectual Property India has published a patent application (202621049412 A) filed by Alard University, Alard School Of Pharmacy on April 17, 2026, for Novel 4-(hydrazinylphenyl)-6-(substituted Phenyl)pyrimidin-2(1h)-One Derivatives: Synthesis, Characterization, And Therapeutic Applications As Anticancer And Antibacterial Agents.

Inventors include Dr. Ganesh Andhale; Dr. Madhuri Shelar; Mr. Pratik Tak; Prof. Sapana Nagare; Dr. Sohan Chitlange; Prof. Ashwini Kshirsagar; Prof. Ashlesha Kohale; Prof. Pallavi Kaple; and Prof. Kirti Sahu.

The application for the patent was published on June 12, 2026, under issue no. 24/2026.

Abstract: ABSTRACT The present invention relates to novel pyrimidine derivatives of the general formula 4-(hydrazinylphenyl)-6-(substituted phenyl)pyrimidin-2(1H)-one (Compounds A1–A4), their synthesis, characterization, and pharmacological applications. The compounds are synthesized by a three-step route involving Claisen– Schmidt condensation of substituted benzaldehydes with acetophenone, cyclization with urea to form the pyrimidinone scaffold, and hydrazinolysis to introduce the hydrazinyl pharmacophore. Comprehensive characterization was performed by melting point, TLC, FT-IR, 1H NMR, 13C NMR, and LC-MS spectral analysis. In silico evaluation by SwissADME confirmed Lipinski compliance and high GI absorption for all compounds. Molecular docking against the 5NQR receptor demonstrated binding affinities of -9.5, -9.0, -9.3, and -9.7 kcal/mol for A1–A4 respectively. In vitro MTT cytotoxicity assay against MCF-7 breast cancer cells revealed IC50 values of 245.75, 303.60, 244.57, and 251.94 µg/mL for A1–A4 respectively, with Cisplatin (IC50 = 187.03 µg/mL) as standard. Antibacterial testing by agar well diffusion demonstrated significant activity of A1 and A3 against Staphylococcus aureus (zones of inhibition: 12.5 mm and 12.4 mm) and moderate activity against Escherichia coli. The invented compounds represent promising lead candidates for further development as anticancer and antibacterial therapeutic agents.

Disclaimer: Curated by HT Syndication.