Synthesis, Antibacterial, and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives using Vilsmeier Reagent

Abstract

Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl)amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones (5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones was secerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds (5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.

Assessment Of Phytochemical Constituent And Antioxidant Capacities Of Ricinus Communicus Seed Extracts

“…This research aims to increase awareness regarding antioxidants while finding methods for improving their beneficial effects 20 . free radicals and their associated species can cause severe impairment in biomolecule cells, proteins, lipids, Deoxyribonucleic Acid, and celluloses resulting in damage the cell 21 . Antioxidants are necessary because they destroy free radicals, lessen the effects of oxidative stress, and have the potential to inhibit the development of certain diseases, including those that are associated with aging, cardiac issues, and cancer.…”