[Et₃NH][HSO₄]-Catalyzed One-Pot Solvent Free Syntheses of Functionalized [1,6]-Naphthyridines and Biological Evaluation

Abstract

We have developed a convenient one-pot multicomponent synthesis of highly functionalized [1,6]-naphthyridines under solvent free condition using [Et₃NH][HSO₄] in excellent yield. This protocol offers several advantages, including short reaction time, simple experimental workup procedure and no toxic byproducts, avoids the use of toxic organic solvents and anhydrous conditions. Further. we have screened the synthesized naphthyridines for in vitro antibacterial, antifungal and antioxidant activity. Furthermore, a molecular docking study of these compounds was carried out to investigate their binding pattern with the target, β-Ketoacyl-acyl carrier protein synthase III (FabH). Finally, the ADME parameters for these compounds showed good drug like properties and can be developed as oral drug candidates.

Keywords:

• Antimicrobial
• Antioxidant
• FabH
• ADME
• Naphthyridines
• [Et₃NH][HSO₄]
• multicomponent reactions

Acknowledgement

The authors M.H.S. and D.D.S. are very much grateful to the Council of Scientific and Industrial Research (CSIR), New Delhi for the award of Senior Research Fellowship. Authors are also thankful to the University Grants Commission and Department of Science & Technology, New Delhi for financial support under UGC-SAP and DST-FIST schemes. Authors also thank Schrodinger Inc. for GLIDE software to perform the molecular docking studies.

Disclosure statement

No potential conflict of interest was reported by the authors.