483287-97-4

Upstream product

• 54903-22-9 6-[3-(4-chloro-phenyl)-acryloyl]-3H-benzooxazol-2-one 
• 54903-09-2 6-acetyl-3H-benzooxazol-2-one 
• 59-49-4 2-Benzoxazolinone 

Downstream Products

• 1207378-81-1 11-(4-chlorophenyl)-7,8-dimethoxy-10-methyl-1,11-dihydro-2H-[1,3]-oxazolo[4',5':5,6] 
• 483287-99-6 5-(4-chlorophenyl)-3H-indeno[5,6-d]oxazol-2,7-dione 
• 483287-98-5 6-bromo-5-(4-chlorophenyl)-3H-indano[5,6-d]oxazol-2,7-dione 
• 483288-01-3 5-amino-3-(4-chlorophenyl)-6-hydroxyindan-1-one 

Relevant academic research and scientific papers

Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands

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

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.

Investigations of new lead structures for the design of novel cyclooxygenase-2 inhibitors

On the basis of molecular modelling studies, five new compounds were synthesised and studied in an attempt to design new lead structures as selective COX-2 inhibitors.