55276-42-1Relevant articles and documents
Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities
Lapmanee, Sarawut,Palavong, Nitwaree,Reamtong, Onrapak,Ruchirawat, Somsak,Thongsornkleeb, Charnsak,Tummatorn, Jumreang
supporting information, p. 1449 - 1458 (2021/09/13)
A new synthetic method for the construction of benzoazepine analogues has been developed employing ortho-arylmethylbenzyl azide derivatives as precursors using an azide rearrangement reaction. In this work, 14 benzoazepine compounds were successfully synthesized in moderate to excellent yields. All synthetic benzoazepines were evaluated for their cytotoxicity against normal human kidney cell line (HEK cell). The results showed that compound 18c had the lowest cytotoxicity (IC50 = 65.68 μM) among tested compounds, which was comparable with the antianxiety drug diazepam (IC50 = 87.90 μM). Based on the cytotoxicity results, five benzoazepine analogues (compounds 18c, 18h, 18j, 18n, and 18p) were selected to determine the antianxiety effect on stressed rats using elevated plus maze (EPM) and open field test (OFT) methods. Interestingly, compound 18c showed better anxiolytic activity than diazepam without a sedative effect by showing superior hyperlocomotor activity. Therefore, this discovery could pave the way for drug development to treat patients with anxiety disorder.
PYRAZOLE COMPOUNDS ACTING AGAINST ALLERGIC, INFLAMMATORY AND IMMUNE DISORDERS
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Page/Page column 41-42, (2012/05/05)
The present invention relates to pyrazole amide derivatives pharmaceutical compositions containing these compounds and to their use in therapy.
N-PYRAZOLYL CARBOXAMIDES AS CRAC CHANNEL INHIBITORS
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Page/Page column 46, (2010/11/05)
The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.