Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Structure-Activity Evaluation of N-benzyl-5-substituted Indole-3-imine Derivatives and their Amine Congeners as Bovine Testicular Hyaluronidase (BTH) Inhibitor

Author(s): S. Olgen, A. Kaessler, Z. Kilic Kurt, J. Jose.


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.

Keywords: Hyaluronidase, Indole derivatives, Inhibition, Morgan-Elson assay, Stains all assay, Structure-activity, glycosaminoglycanes, HA fragments, extracellular matrix, opthalmology, lanostanoids, Vilsmeir formylation reaction, Schiff bases, Stains-all Assay

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Article Details

Year: 2011
Page: [685 - 690]
Pages: 6
DOI: 10.2174/157018011796576079
Price: $58