الفهرس | Only 14 pages are availabe for public view |
Abstract Considering the several theories and suggestions enlightening the relevance and design of novel compounds that are used as β-adrenergic blockers, assisted by a comprehensive literature survey on the importance of β-adrenergic blockers as therapy for many diseases. Compounds containing oxime ether moieties in their structures give good β-blocking activity; the synthesis of novel series of compounds that carry the main structural features contributing to β-adrenergic blockers was promoted, aiming to attain more potent and less toxic drugs.In the present investigation, new series of O-(3-alkylamino-2-hydroxypropyl)oxime derivatives were prepared.In order to obtain the target compounds, different chemical pathways were adopted and found to be successful. In the present study, twenty six novel compounds that are not mentioned in the available literature were synthesized. New intermediates were also synthesized guided by the published literature. The formation and purity of the newly synthesized compounds were checked by TLC, and their structures were elucidated through elemental microanalyses, 1H-NMR and mass spectroscopy.Sixteen the newly synthesized compounds were subjected to an in vitro screening for β1-adrenoceptor antagonistic activities using isolated atria of guinea pigs. Besides, eleven of the newly synthesized compounds were subjected to an in vitro screening for β2-adrenoceptor antagonistic activities using isolated trachea of guinea pigs. All the newly synthesized compounds were subjected to molecular docking studies of oxime ether compounds on β2-adrenergic receptor to illustrate the binding forces involved. Most of compounds showed energy of interactions compared to that of reference compounds epinephrine, salbutamol, propranolol, falintolol and IPS 339 |