title: Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.
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.
authors: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors: Parteek
authors: P
authors: Prasher
authors: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors: Pooja
authors: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: palwinder_singh_2000@yahoo.com.
authors: Palwinder
authors: P
authors: Singh
mesh_terms: D000596:Amino Acids; D007211:Indoles / Q000494:pharmacology*; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology*; D008958:Models, Molecular; D062105:Molecular Docking Simulation; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D007211:Indoles; D016859:Lipoxygenase Inhibitors
keywords: 5-LOX inhibition; Amino acid; Indole; Molecular modeling