140382-29-2Relevant articles and documents
Synthesis and antidepressant activity of 5-(benzo[b]furan-2-ylmethyl)-6-methylpyridazin-3(2H)-one derivatives
Boukharsa, Youness,Meddah, Bouchra,Tiendrebeogo, Ramata Yvette,Ibrahimi, Azeddine,Taoufik, Jamal,Cherrah, Yahia,Benomar, Ali,Faouzi, My El Abbes,Ansar, M'Hammed
, p. 494 - 500 (2016)
A new series of pyridazin-3-one derivatives were designed, synthesized and evaluated for their preclinical antidepressant effect on Swiss mice. Among the series, compounds 6c, 6d and 6f exhibited significant activity profile in forced swimming test. Compounds 6c and 6d were most efficacious, which at dose of 50 mg kg-1 reduced the time of immobility by 42.85 and 38.09 %, respectively, as compared to the standard drug fluoxetine which reduced the immobility time by 45.23 % at the dose of 32 mg kg-1. All the test and standard compounds were administered orally 60 min before the test. Interestingly, all active compounds did not cause any significant alteration of locomotor activity in mice as compared to control, indicating that the hybrids did not produce any motor impairment effects. The results indicate that pyridazin-3(2H)-one derivatives may have potential therapeutic value for the management of mental depression.
Efficient synthesis of chiral benzofuryl β-amino alcohols via a catalytic asymmetric Henry reaction
Chen, Wei,Zhou, Zhao-Hui,Chen, Hong-Bin
, p. 1530 - 1536 (2017/02/15)
Chiral β-amino alcohol ligands were found effective for the copper(ii)-catalyzed asymmetric Henry reaction of benzofuran-2-carbaldehydes with nitromethane, which led to the formation of (S)-enriched benzofuryl β-nitro alcohols with satisfactory enantioselectivities (up to 98% ee). Using this catalytic protocol, bioactive (S)-benzofuryl β-amino alcohols could be conveniently prepared in short steps.
