Inhibitory Activities of Pyrazolo-Oxazine Heterocyclic Derivatives

Despite several reports and reviews addressing the biological significance of pyrazoles and oxazines, no comprehensive work on the pyrazolo oxazine fused ring system has been published so far.We report all biological evaluations on pyrazolo-oxazine derivatives in this mini-review to provide an avenue for medicinal and pharmacological researchers to conduct further in-depth exploration.

IN SILICO STUDIES OF N-(PHENYL SUBSTITUTED) 2-([PHENYL SUBSTITUTED) METHYLIDENE] AMINO)-N,4- DIPHENYL-6H-1,3-OXAZIN-6-AMINE DERIVATIVES AS POTENTIAL ANTIBACTERIAL AGENTS

Resistance to bacteria is a growing threat to human health worldwide. The rate of discovery of new antibacterial is far outshined by the rate at which resistance is spreading. Therefore, there remains a pressing need for the development of new antibacterial drugs. Recent alarm estimates that deaths due to antimicrobial resistance may increase from 700,000 million lives annually by 2050. Glucosamine-6-phosphate (GlcN-6-P) synthase represents an interesting protein target because it plays an essential role in the protection of cell wall. The primary aim and objective of this study is to identify lead molecules as promising antibacterial agents by inhibiting Glucosamine-6-phosphate (GlcN-6-P) synthase enzyme. Autodock 4. 2, the effective tool for exploring the binding affinity of small molecule to enzyme target was used to study the interactions between the oxazine derivatives and the GlcN-6-P synthase binding site. The ligands were optimized for improving their efficacy and safety. Lead optimization was performed using Molinspiration server and the ligands were optimized for evaluating their oral bioavailability. With Glucosamine 6 phosphate synthase receptor, the binding energy was found to be best for 5 compounds SZ-3 (-5.27 kcal/mol), SZ-4 (-6.02 kcal/mol), SZ-5 (-5.35 kcal/mol), SZ-8 (-5.62kcal/mol), SZ-10 (-5.29 kcal/mol) when compared to the standard ligand, Ciprofloxacin (-5.09 kcal/mol) and were interacting well with the key residues TYR 304, GLU 438, LEU 484. Docking study strongly enhanced the activity of oxazine derivatives as new discovered hits.

Facile access to [1,2]-oxazine derivatives via annulations of aminoxy-tethered 1,7-enynes

Highly diastereoselective construction of functionalized cyclopenta[d][1,2]oxazines is achieved from 1-aryl propargyl alcohols via sequential oxyamination/annulation reactions.

Syntheses, Biological and Material Significance of Dihydro[1,3]oxazine Derivatives: An Overview

: Dihydro[1,3]oxazines are an important class of heterocyclic compounds having a wide range of biological and material properties. Medicinally, they possess diverse pharmacological activities such as bactericidal, fungicidal, microbiocidal, antitumor, anti-HIV and anti-inflammatory agents. Apart from being biologically active, they are materially useful for making polybenzoxazines. Polybenzoxazines, a novel class of non-conjugated thermosetting materials that belong to the family of addition-curable phenolic resins. They have lucrative properties such as small shrinkage in curing, low water absorption, good thermal stability, no release of volatile materials during cure, no need for catalyst and inexpensive raw materials. Further, the flexibility in designing a monomer gives polybenzoxazines an additional edge over ordinary phenolic resins. This review briefly describes the syntheses including eco-friendly strategies, biological and material significance of various dihydro[1,3]oxazine derivatives.

Green Chemistry Synthesis Methods of Oxazine and Thiazine Derivatives as Promising Scaffolds in Medicinal Chemistry: A Mini-Review

: Green synthesis of oxazine and thiazine derivatives have concerned a great impact of concern of medicinal researchers and provided a lead molecule for the design and development of various potential bioactive molecules. This review associated additional green synthetic information and it would extend a great deal of help to researchers in synthesizing the most productive, economical, and clinically important thiazine and oxazine derivatives which will be expected to show potent pharmacological activities. This has led to the discovery of various compounds that have diverse types of interesting biological activities. Propose of this article is to study the various synthetic methods of oxazine and thiazine derivatives by green chemistry methods and their biological activities. We expect that this article will be interesting for researchers concerned with oxazine and thiazine compounds.