89266-23-9Relevant academic research and scientific papers
MAO Inhibitory Activity of 2-Arylbenzofurans versus 3-Arylcoumarins: Synthesis, invitro Study, and Docking Calculations
Ferino, Giulio,Cadoni, Enzo,Matos, Maria Joao,Quezada, Elias,Uriarte, Eugenio,Santana, Lourdes,Vilar, Santiago,Tatonetti, Nicholas P.,Yanez, Matilde,Vina, Dolores,Picciau, Carmen,Serra, Silvia,Delogu, Giovanna
, p. 956 - 966 (2013/07/27)
Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. Several 3-arylcoumarin derivatives were previously described as interesting selective MAO-B inhibitors. Preserving the trans-stilbene structure, a series of 2-arylbenzofuran and corresponding 3-arylcoumarin derivatives were synthesized and evaluated as inhibitors of both MAO isoforms, MAO-A and MAO-B. In general, both types of derivatives were found to be selective MAO-B inhibitors, with IC50 values in the nano- to micromolar range. 5-Nitro-2-(4-methoxyphenyl)benzofuran (8) is the most active compound of the benzofuran series, presenting MAO-B selectivity and reversible inhibition (IC50=140nM). 3-(4′-Methoxyphenyl)-6-nitrocoumarin (15), with the same substitution pattern as that of compound 8, was found to be the most active MAO-B inhibitor of the coumarin series (IC50=3nM). However, 3-phenylcoumarin 14 showed activity in the same range (IC50=6nM), is reversible, and also severalfold more selective than compound 15. Docking experiments for the most active compounds into the MAO-B and MAO-A binding pockets highlighted different interactions between the derivative classes (2-arylbenzofurans and 3-arylcoumarins), and provided new information about the enzyme-inhibitor interaction and the potential therapeutic application of these scaffolds.
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal
Pereira, Alban R.,Strangman, Wendy K.,Marion, Frederic,Feldberg, Larry,Roll, Deborah,Mallon, Robert,Hollander, Irwin,Andersen, Raymond J.
supporting information; experimental part, p. 8523 - 8533 (2011/02/26)
Analogues of the sponge meroterpenoid liphagal (1) have been synthesized and evaluated for inhibition of PI3Kα and PI3Kα as part of a program aimed at developing new isoform-selective PI3K inhibitors. One of the analogues, compound 24, with IC50/sub
FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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Page/Page column 325, (2008/06/13)
The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.
Novel benzofuran derivatives for PET imaging of β-amyloid plaques in Alzheimer's disease brains
Ono, Masahiro,Kawashima, Hidekazu,Nonaka, Akemi,Kawai, Tomoki,Haratake, Mamoru,Mori, Hiroshi,Kung, Mei-Ping,Kung, Hank F.,Saji, Hideo,Nakayama, Morio
, p. 2725 - 2730 (2007/10/03)
A novel series of benzofuran derivatives as potential positron emission tomography (PET) tracers targeting amyloid plaques in Alzheimer's disease (AD) were synthesized and evaluated. The syntheses of benzofurans were successfully achieved by an intramolec
Research on nitro derivatives of biological interest. XXXIII. Synthesis and action on microorganisms of 5-nitrofurylic and 5-nitro thienylic benzofuran derivatives
Guillaumel,Royer,Le Corre,et al.
, p. 431 - 436 (2007/10/02)
Quite a number of benzofurans substituted at the 2-position by a 5-nitrofuryl, 5-nitrothienyl, 5-nitro 2-furyl ethenyl or 5-nitro 2-thienyl ethenyl group were prepared by heterocyclization of 2-acyloxy benzyltriphenylphosphonium bromides derivated from 2-hydroxy benzyl triphenylphosphonium bromides, themselves obtained by action of triphenylphosphine bromhydrate on ortho hydroxylated benzyl alcohols. Besides, several 5-nitro 2-furoyl benzofurans were also obtained by condensation of diversely substituted salicylaldehydes and 2-bromacetyl 5-nitrofuran. Most of these new benzofuran heterocyclic nitro derivatives are deprived of the parasiticidic and antibacterial properties owned by 2-nitro benzofurans.
