103680-87-1Relevant articles and documents
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids
Sun, Yang,Chen, Jianwen,Chen, Xuemin,Huang, Ling,Li, Xingshu
, p. 7406 - 7417 (2013/11/19)
A series of Tacrine-Homoisoflavonoid hybrids were designed, synthesised and evaluated as inhibitors of cholinesterases (ChEs) and human monoamine oxidases (MAOs). Most of the compounds were found to be potent against both ChEs and MAO-B. Among these hybrids, compound 8b, with a 6 carbon linker between tacrine and (E)-7-hydroxy-3-(4-methoxybenzylidene)chroman-4-one, proved to be the most potent against AChE and MAO-B with IC50 values of 67.9 nM and 0.401 μM, respectively. This compound was observed to cross the blood-brain barrier (BBB) in a parallel artificial membrane permeation assay for the BBB (PAMPA-BBB). The results indicated that compound 8b is an excellent multifunctional promising compound for development of novel drugs for Alzheimer's disease (AD).
A NEW SYNTHESIS OF HOMOISOFLAVANONES (3-BENZYL-4-CHROMANONES)
Jain, Amolak C.,Mehta, Anita
, p. 5933 - 5938 (2007/10/02)
Two 7-hydroxyhomoisoflavanones (6a/6b) have been synthesized from corresponding 2'-hydroxydihydrochalcones (2a/2b) in about 33percent overall yields.The stages are : (i) selective protection of C4'-hydroxyl in 2a/2b with EtO.CH2Cl (1 molar equiv.) in the
A New Synthesis of Homoisoflavanones (3-Benzyl-4-chromanones)
Jain, A. C.,Mehta, Anita
, p. 1170 - 1171 (2007/10/02)
7-Hydroxy-4'-methoxyhomoisoflavanone (5) has been synthesised from 2',4'-dihydroxy-4-methoxydihydrochalcone (1) by a new method involving ethoxymethylation of 4'-hydroxyl group to give 2, followed by hydroxymethylation of the bridge methylene in 2, heterocyclization of 3 and deprotection of 4.