Novel phospha-oxazepinoquinazolinyl derivatives of ibuprofen as nitric oxide synthase inhibitors: Synthesis and biological evaluation

The in vitro biological assessment of novel hybrid phospha-oxazepino derivatives bearing ibuprofenyl quinazolinone moiety as preventing stroke symptoms and inhibitors of nitric oxide synthase (iNOS and nNOS) isoforms was described. In general, products tested exhibited iNOS inhibition than nNOS. The phosphaoxazepinoquinazolinyl derivatives (4, 7, 10-12) are among the most effective inhibitors of all compounds tested, being also endowed with iNOS over nNOS selectivity. The structures of these new heterocycles were elucidated using spectral data and elemental analysis. (c) 2021 The Authors. Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

Automated summary

This study described the in vitro biological assessment of novel hybrid phospha-oxazepino derivatives bearing ibuprofenyl quinazolinone moiety as preventing stroke symptoms and inhibitors of nitric oxide synthase (iNOS and nNOS) isoforms. Overall, the tested products exhibited greater inhibition of iNOS than nNOS. The phosphaoxazepinoquinazolinyl derivatives (4, 7, 10-12) were found to be among the most effective inhibitors, showing selectivity for iNOS over nNOS.