Discovery of bisindolyl-substituted cycloalkane-anellated indoles as novel class of antibacterial agents against S. aureus and MRSA

El-Sayed M. T., SÜZEN S., ALTANLAR N., Ohlsen K., Hilgeroth A.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.26, sa.1, ss.218-221, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 26 Sayı: 1
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1016/j.bmcl.2015.10.085
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.218-221
  • Anahtar Kelimeler: Cycloalkane indoles, Antibacterial activity, MRSA, Structure-activity relationships, RESISTANCE
  • Ankara Üniversitesi Adresli: Evet

Özet

Antibiotic resistance is an ongoing problem in the treatment of bacterial diseases. Among the various antibacterial infections Staphylococcus aureus infections remain critical due to the increasing resistances, especially against the methicillin-resistant S. aureus (MRSA). We discovered novel antibacterial compounds with activities against both S. aureus and MRSA types. Structure-activity relationships (SAR) are discussed and show that the activity depends on the ring size of the anellated cycloalkane. Moreover, first substituent effects have been investigated for both the cycloalkane and the indole residues. (C) 2015 Elsevier Ltd. All rights reserved.