Structure-activity evaluation of n-benzyl-5-substituted indole-3-imine derivatives and their amine congeners as bovine testicular hyaluronidase (BTH) inhibitor

Ölgen S., Kaessler A., KILIÇ KURT Z., Jose J.

Letters in Drug Design and Discovery, cilt.8, sa.9, ss.685-690, 2011 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 8 Sayı: 9
  • Basım Tarihi: 2011
  • Dergi Adı: Letters in Drug Design and Discovery
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.685-690
  • Anahtar Kelimeler: Hyaluronidase, Indole derivatives, Inhibition, Morgan-Elson assay, Stains all assay, Structure-activity
  • Ankara Üniversitesi Adresli: Evet

Özet

With the aim to overcome the lack of potent and selective Hyaluronidases (Hyals) inhibitors, we have tested new 1, 3 and 5 substituted indole derivatives for the inhibition of bovine testicular hyaluronidases (BTH) in a stains-all assay at pH 7 and in a Morgan-Elson assay at pH 3.5. Most of the compounds are found as activator at pH 3.5. Although amine compounds 17 and 18 did not show inhibition of BTH at pH 7, they reacted as most potent activators of BTH at pH 3.5. On the other hand, some of the imine compounds reacted as the inhibitors at pH 7 and compound 25 was found as the most potent inhibitor. © 2011 Bentham Science Publishers Ltd.