Indole derivatives as potent inhibitors of 5-lipoxygenase: Design, synthesis, biological evaluation, and molecular modeling

Design, synthesis of novel N prenylated indole-3-carbazones and evaluation of in vitro cytotoxicity and 5-LOX inhibition activities

“…Therapeutic potential of 5-LOX inhibition has been widely highlighted in recent years (Balkan and Berk, 2003;Funk, 2005;Yoshimura et al, 2005). Literature survey reveals N-1 and C-3 substituted indoles are identified as 5-LOX inhibitors (Prasher et al, 2014;Singh and pooja, 2013;Zheng et al, 2007). Based on the literature survey the novel 1-(5-substituted-1-(3-methylbut-2-enyl)-1H-indole-3-yl) methylene) carbazides (5a-f) were screened for their inhibitory properties against 5-LOX enzyme employing the assay described by Reddanna et al, 1990.…”

Biological importance of the indole nucleus in recent years: A comprehensive review

“…synthesized a series of indole derivatives as possible 5‐lipoxygenase inhibitors. In all, four compounds 24 , 25 , 26 , and 27 exhibited the most potent inhibitory activity with IC 50 values ranging from 0.74 μ M to 3.17 μ M [14]. …”

Synthesis of mono, bis-2-(2-arylideneaminophenyl) indole azomethines as potential antimicrobial agents

“…Indole derivatives offer a high degree of structural diversity and have proven to be broadly useful as therapeutic agents. Usually, indole and its analogs constitute the active class of compounds possessing a wide spectrum of biological activities, such as antiinflammatory (Zheng et al, 2007), antimicrobial (Gurkok et al, 2009), antibacterial (Sharma et al, 2006), anticonvulsant (Gitto et al, 2009) and cardiovascular (Yorikane et al, 1991). In fact, a number of drugs such as indolmycin (Hurdle et al, 2004), reserpine (Krönig et al, 1997), vincristine (Mihelic et al, 2007), the 5-HT3 receptor antagonist ondansetron (Clavel et al, 1995) and 5HT1 receptor agonist sumatriptan (Sakai et al, 2008) have an indole nucleus in their structures.…”