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Bioorg Med Chem. 2014 Mar 1;22(5):1642-8. doi: 10.1016/j.bmc.2014.01.027. Epub 2014 Jan 29.

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

Author information

1
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
2
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: palwinder_singh_2000@yahoo.com.

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.

KEYWORDS:

5-LOX inhibition; Amino acid; Indole; Molecular modeling

PMID:
24508141
DOI:
10.1016/j.bmc.2014.01.027
[Indexed for MEDLINE]

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