Biological Activity of the Hypolipidemic Agent, N2-n-Butylindazolone

Photocatalyst‐free Synthesis of Indazolones under CO2 Atmosphere

“…Simple primary and secondary alkyl amines reacted with 2‐nitrobenzyl alcohol giving rise to 4 a – 4 e in moderate to good yield (58–85 %). Notably, 4 b was found to be effective as an inhibitor in both 5‐lipoxygenme (5‐LPO) and cyclooxygenase (CO) by oral dose . The present one‐operation procedure (63 %) is operationally simple and provides an efficient method with high atom‐economy in comparison with the reported method (see SI) .…”

“…Notably, 4b was found to be effective as an inhibitor in both 5lipoxygenme( 5-LPO) and cyclooxygenase (CO) by oral dose. [3,4] The presento ne-operation procedure (63 %) is operationally simplea nd provides an efficient methodw ith high atom-economy in comparison with the reported method( see SI). [14] Although, tert-butylamine gave no desired productd ue to the steric hindrance, laurylamine having al ong carbon chain gave an excellent yield (4f,8 0%).…”

“…Indazolones are attractive heterocyclic compounds possessing high bioactivities . Therefore, we selected 28 compounds in 100 μ m and subjected them to preliminary screening for anticancer activities in Hela (human cervical cancer cell), EJ and MDA‐MB‐231, MCF‐7 (human breast cancer cell), PC‐3 and U87.…”

“…Indazolones [1] attract attention by their biological activities ( Figure 1), and their heterocyclic skeleton was found in anti-inflammatory agents, [2] 5-lipoxygenase inhibitors, [3] hypolipidemic agents (N 2 -h-butylindazolone) [4] or antitumora gentsi nh uman tumor cells. [5] Until recently,f our synthetic routes fori ndazolones were known as shown in Scheme 1(a-d).…”

Indazole: a medicinally important heterocyclic moiety

“…The lipid contents of the liver, small intestine, and serum lipoprotein fractions were decreased, whereas the lipid content was increased in fecal excretions by drug treatment for 14 h. The absorption of the orally administered cholesterol from the intestine was reduced after drug administration (Hall et al, 1984).…”