Recent advances in the synthesis, reaction, and bio-evaluation potential of purines as precursor pharmacophores in chemical reactions: a review

RSC Advances, Journal Year: 2025, Volume and Issue: 15(5), P. 3607 - 3645

Published: Jan. 1, 2025

Purines as precursor pharmacophores in chemical reactions.

Language: Английский

Synthesis, Anti-Inflammatory, and Molecular Docking Studies of New Heterocyclic Derivatives Comprising Pyrazole, Pyridine, and/or Pyran Moieties

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(3), P. 335 - 335

Published: Feb. 26, 2025

Introduction: Inhibiting cyclooxygenase-2 (COX-2) is a potential strategy in inflammation therapy. Thus, developing COX-2 inhibitors plays pivotal role efficient treatment. This study discloses the synthesis of new heterocyclic compounds incorporating pyridine, pyran, and/or pyrazole moieties as inhibitors. Methods: In this study, Claisen–Schmidt reaction 1-(5-hydroxy-1,3-diphenyl-1H-pyrazol-4-yl)ethan-1-one 1 and p-methoxybenzaldehyde ethanol containing aqueous sodium hydroxide (10%) led to formation 1-(5-hydroxy-1,3-diphenyl-1H-pyrazol-4-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) 2. The latter compound was allowed react key precursor with various nucleophiles such ethyl cyanoacetate, malononitrile, cyclohexanone, acetoacetate, hydrazine, cyano acid hydrazide, thiosemicarbazide yield derivatives comprising 3–15, according Michael addition reaction. newly synthesized were depicted using spectroscopic techniques IR, 1H-NMR, 13C-NMR, MS. Moreover, their anti-inflammatory efficiency vitro evaluated by means protein denaturation inhibition cell membrane protection assay. Results: results 2−ΔΔct values expression for 6, 11, 12, 13 6.6, 2.9, 25.8, 10.1, respectively. Therefore, followed 13, showed potent properties evaluation. Further, an silico molecular docking performed on best-docked reference drug (Diclofenac) investigate binding affinities against active site target enzyme. obtained from aligned biological Conclusions: studies open doors designing heterocycles agents.

Language: Английский

Design and synthesis of new 1,4-naphthoquinones appended sulfenylated thiazoles as cyclooxygenase II inhibitors: Exploring the utility in the development of anticancer agents

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 161, P. 108537 - 108537

Published: April 26, 2025

Language: Английский