Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.

Basic Information

ID: ALA3112507

Journal: Bioorg Med Chem

Title: Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.

Authors: Prasher P, Pooja, Singh P.

Abstract: N-1 tosyl indoles carrying amino acid as a part of C-3 substituent are identified with considerable 5-LOX inhibitory activities. On the basis of enzyme inhibitory activities and logP, it is found that these compounds are more suitable to use as ester prodrugs. In addition to the significant Ka and Ki for 5-LOX, advantageously the compounds under present investigation do not affect the viability of the cell. The experimental results were also supported by molecular docking of compounds in the active site of 5-LOX.

CiteXplore: 24508141

DOI: 10.1016/j.bmc.2014.01.027

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