oxalates and oxamide

In this study, a range of oxamide ligands were synthesized by the reaction of amines with oxalyl chloride in basic medium. Spectroscopic and analytical techniques such as IR, 1H-NMR and ESI-MS techniques were used for characterization of the synthesized oxamides. The synthesized oxamides were screened for Lipoxygenase inhibition. Biological screening revealed that the oxamides possessed good lipoxygenase inhibition activities, whereas, the unsubstituted oxamide did not show any distinct lipoxygenase inhibition activity. Molecular docking studies of the oxamides were also carried out for lipoxygenase inhibition. The results obtained from molecular docking were well correlated with the empirical data.

Topics: Amines; Arachidonate 5-Lipoxygenase; Chlorides; Drug Evaluation, Preclinical; Lipoxygenase Inhibitors; Magnetic Resonance Spectroscopy; Molecular Docking Simulation; Oxalates; Oxamic Acid; Protein Conformation; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship

The development of biodegradable and biocompatible materials is the basis for tissue engineering and drug delivery. The aims of this study are to develop the poly(oxalate-co-oxamide) (POXAM) and evaluate its physicochemical properties and biocompatibility as the initial step for the development of new biomaterials. POXAM had a molecular weight of ~70,000 Da and rapidly degraded under physiological condition with a half-hydrolysis of ~4 days. POXAM films exhibited relative hydrophilic nature because of the presence of oxamide linkages and induced a higher cell attachment and proliferation compared with poly(lactic-co-glycolic acid) (PLGA) films. In vitro inflammatory responses to POXAM were evaluated using murine macrophage RAW 264.7 cells. POXAM films minimally stimulated the cells to generate less production of tumor necrosis factor-alpha (TNF-α) than PLGA films. We assessed the in vivo inflammatory responses to POXAM films implanted in the dorsal skin of rats. Histological studies revealed that POXAM provoked remarkably reduced inflammatory responses, evidenced by the less accumulation of inflammatory cells and giant cells, thinner fibrotic capsules, in comparison with PLGA. Given its excellent biocompatibility, fast degradation, and very mild inflammatory responses, POXAM has great potential for biomedical applications, such as scaffolds, wound dressing, and fast drug delivery.

Topics: Animals; Biocompatible Materials; Cell Line; Implants, Experimental; Lactic Acid; Macrophages; Materials Testing; Mice; Molecular Structure; Oxalates; Oxamic Acid; Polyglycolic Acid; Polylactic Acid-Polyglycolic Acid Copolymer; Rats; Rats, Wistar

Schiff bases derived from oxaldiamide/oxalylhydrazine and pyrrol-2-carbaldehyde, or salicylaldehyde respectively, as well as their Zn(II) complexes have been prepared and tested as antibacterial agents. These Schiff bases function as tetradentate ligands, forming octahedral Zn(II) complexes. The ketonic form for the diamide derived Schiff base and the enolic form of the hydrazide derived Schiff base were the preferred tautomers for coordination of the metal ions. The title compounds and their Zn(II) derivatives were evaluated for antibacterial activity against several bacterial strains which easily develop resistance to classical antibiotics, such as Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa. Some of them showed promising biological activity in inhibiting the growth of such organisms.

Topics: Aldehydes; Anti-Bacterial Agents; Bacteria; Microbial Sensitivity Tests; Organometallic Compounds; Oxalates; Oxamic Acid; Pyrroles; Schiff Bases; Structure-Activity Relationship; Zinc

The direct intramedullary inoculation of stable L-phase variants of Staphylococcus aureus failed to colonize normal and hydronephrotic rat kidneys induced by oral feeding of oxamide.

Topics: Amides; Animals; Hydronephrosis; Kidney Medulla; L Forms; Male; Oxalates; Oxamic Acid; Rats; Staphylococcus; Urine

Topics: Amides; In Vitro Techniques; Oxalates; Oxamic Acid; Pharmacology; Photomicrography; Rats; Research; Surgical Procedures, Operative; Urinary Calculi; Urolithiasis; Urologic Diseases

Topics: Hydantoins; Imidazoles; Oxalates; Oxamic Acid; Ultraviolet Rays; Uracil