Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors
Parteek Prasher1, Pooja1, Palwinder Singh1
1Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
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.
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