54903-22-9Relevant academic research and scientific papers
Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands
Donnier-Maréchal, Marion,Larchanché, Paul-Emmanuel,Le Broc, Delphine,Furman, Christophe,Carato, Pascal,Melnyk, Patricia
, p. 198 - 206 (2014/12/11)
Sigma 1 receptors are associated with neurodegenerative and psychiatric disorders. These receptors, via their chaperoning functions that counteract endoplasmic reticulum stress and block neurodegeneration, may serve as a target for a new generation of antidepressants or neuroprotective agents. The involvement of these receptors has also been observed in neuropathic pain and cancer. Only a few ligands, such as Igmesine and Anavex 2-73, have been involved in clinical trials. Thus the development of sigma 1 ligands is of interest to a new generation of drugs. Previous work in our lab underlined the potency of benzannulated bicyclic compounds as interesting ligands. Herein the work was extended to a series of novel tricyclic compounds. Carboline- and phenothiazine-derivated compounds were designed and synthesized. In vitro competition binding assays for sigma 1 and 2 receptors showed that most of them have high affinity for sigma 1 receptor (Ki = 2.5-18 nM), and selectivity toward sigma 2 receptor, without cytotoxic effects on SY5Y cells.
Synthesis of 1,11-dihydro-2H-[1,3]oxazolo[4′,5′:5,6]indeno[1,2- b]quinolin-2-ones with potential topoisomerase I inhibitory activity
Delot, Marc,Carato, Pascal,Furman, Christophe,Lemoine, Amelie,Lebegue, Nicolas,Berthelot, Pascal,Yous, Said
scheme or table, p. 3819 - 3822 (2010/03/03)
A series of 1,11-dihydro-2,11-[1,3]oxazolo[4′,5′:5,6]indeno[1, 2-b]quinolin-2-ones were prepared by means of Friedlaender condensations. The starting materials for the preparations were commercial substituted-2- aminoacetophenones and various 5,6-dihydro-2H-indeno[5,6-d][l,3]oxazole-2,7(3H)- diones that were synthesized from 2(3H)-benzoxazolones or their N-methyl analogues. Thieme Verlag Stuttgart.
6 Acylbenzoxazolinone derivatives. II. Preparation of some transformation products
Bonte,Lesieur,Lespagnol,et al.
, p. 497 - 500 (2007/10/08)
Some transformation products of acylbenzoxazolinones (aminophenols, alcohols, and chalcone derivatives) are described. Preliminary pharmacodynamic study showed analgesic activity.
