2. Academic Validation
  3. Design, synthesis, and evaluation of novel 2-phenylpropionic acid derivatives as dual COX inhibitory-antibacterial agents

Design, synthesis, and evaluation of novel 2-phenylpropionic acid derivatives as dual COX inhibitory-antibacterial agents

  • J Enzyme Inhib Med Chem. 2017 Dec;32(1):732-745. doi: 10.1080/14756366.2017.1310726.
Hülya Karaca Gençer 1,  Ulviye Acar Çevik 2 3,  Betül Kaya Çavuşoğlu 2,  Begüm Nurpelin Sağlık 2 3,  Serkan Levent 2 3,  Özlem Atlı 4,  Sinem Ilgın 4,  Yusuf Özkay 2 3,  Zafer Asım Kaplancıklı 2
Affiliations

Affiliations

  • 1 a Department of Pharmaceutical Microbiology, Faculty of Pharmacy , Anadolu University , Eskişehir , Turkey.
  • 2 b Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Anadolu University , Eskişehir , Turkey.
  • 3 c Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy , Anadolu University , Eskişehir , Turkey.
  • 4 d Department of Pharmaceutical Toxicology, Faculty of Pharmacy , Anadolu University , Eskişehir , Turkey.
PMID: 28413890 DOI: 10.1080/14756366.2017.1310726
Abstract

A series of 2-(4-substitutedmethylphenyl)propionic acid derivatives (6a–6m) were synthesized, characterized and evaluated for cyclooxygenase (COX) enzyme inhibitory and antimicrobial activity. Test compounds that exhibited good COX inhibition and Antibacterial activity were further screened for their cytotoxicity and genotoxicity. Compounds 6h and 6l showed better COX-1 and COX-2 inhibition when compared to ibuprofen. Inhibition potency of these compounds against COX-2 was very close to that of nimesulide. The compounds 6d, 6h, 6l and 6m displayed promising Antibacterial property when compared to chloramphenicol. However, the compound 6l was emerged as the best dual COX inhibitory-antibacterial agent in this study. The ADME prediction of the compounds revealed that they may have a good pharmacokinetic profile. Docking results of the compounds 6h and 6l with COX-1 (PDB ID: 1EQG) also exhibited a strong binding profile.

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Keywords

COX inhibition; Phenylpropionic acid; antibacterial; docking; dual effect.

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