Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase

El-Sayed M. T., Zoraghi R., Reiner N., SÜZEN S., Ohlsen K., Lalk M., ...Daha Fazla

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, sa.6, ss.1666-1671, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 31 Sayı: 6
  • Basım Tarihi: 2016
  • Doi Numarası: 10.3109/14756366.2015.1118685
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1666-1671
  • Anahtar Kelimeler: Antimicrobial compounds, biological activity, indolyl-derived compounds, CATALYZED EFFICIENT, ANTIBIOTICS KILL, PYRUVATE-KINASE, BIS(INDOLYL)METHANES, MECHANISM, BACTERIA, INDOLE
  • Ankara Üniversitesi Adresli: Evet

Özet

Novel bisindolyl-cycloalkane indoles resulted from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRSA PK inhibitors and now report first inhibiting activities. We discuss structure-activity relationships of structurally varied compounds. Activity influencing substituents have been characterized and relations to antibacterial activities of the most active compounds have been proved.