Synthesis, In Vitro Biological Evaluation, and Molecular Docking Studies of Novel Biphenyl Chalcone Derivatives as Antimicrobial Agents

BURMAOĞLU S., Akin Kazancioglu E., Kazancioglu M. Z., ALAGÖZ M. A., Dogen A., Algul O.

Polycyclic Aromatic Compounds, cilt.42, sa.9, ss.5948-5961, 2022 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 42 Sayı: 9
  • Basım Tarihi: 2022
  • Doi Numarası: 10.1080/10406638.2021.1962925
  • Dergi Adı: Polycyclic Aromatic Compounds
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Aerospace Database, Applied Science & Technology Source, CAB Abstracts, Chemical Abstracts Core, Communication Abstracts, Food Science & Technology Abstracts, Metadex, Pollution Abstracts, Veterinary Science Database, Civil Engineering Abstracts
  • Sayfa Sayıları: ss.5948-5961
  • Anahtar Kelimeler: Antimicrobial activity, biphenyl chalcone, MIC, molecular docking, synthesis, ANTIBACTERIAL, PROTEIN, DESIGN, POTENT
  • Atatürk Üniversitesi Adresli: Evet

Özet

© 2021 Taylor & Francis Group, LLC.The increasing resistance to antimicrobial drugs has instigated the crucial need for the discovery of novel compounds with different modes of action that could target both sensitive and resistant strains. For this purpose, we developed some new chalcone analogs. Herein, a novel series of hybrid biphenyl chalcones (17-24), which have organohalogens in their B ring, were synthesized and examined for their antimicrobial effect. The position of the substituent on ring B was changed to find the effect of the substitution on antimicrobial activity. Compounds 18, 19, and 24 showed better antibacterial and antifungal activity when compared other compounds. Also, molecular docking studies on ATP binding site of S. aureus DNA gyrase for antibacterial targets were performed to elucidate the mechanism of antibacterial activity of synthesized compounds. Three of the most active compounds could be considered as lead compounds for the development of more new potent agents.