Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities.

ABSTRACT: 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 a

SUBMITTER: Reamtong O 

PROVIDER: S-EPMC8436417 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature