No abstract

Depending on the reaction condition, 1-(4-aminosulfonylphenyl)-5-aryl-4-aroyl-3-hydroxy-3-pyrrolin-2-ones reacted with aromatic amines to yield 3-arylamino-3-pyrrolin-2-ones or 4-[aryl (arylamino) methylene]tetrahydropyrrole-2,3-diones. Reactions of 1-(4-aminosulfonylphenyl)-5-aryl-4-aroyl-3-hydroxy-3-pyrrolin-2-ones with hydrazine hydrate afforded pyrrolo[3,4-c]pyrazol-6-ones.

Microbial keratitis (MK) is a homogeneous group of diseases accompanied by loss of the corneal epithelium, stromal leukocyte infiltration and/or destructive tissue breakdown, occurring when the protective mechanisms of the ocular surface are disturbed, which require an immediate set of therapeutic measures, including, first of all, massive etiotropic therapy, which is represented, as a rule, by broad-spectrum antibiotics (AB) and anti-inflammatory drugs. One of the most threatening MK pathogens is P. aeruginosa (PA) (Pseudomonas aeruginosa). Multiple drug resistance, the highest pathogenicity, numerous RA virulence factors dictate the need to search for new highly effective methods to combat MC, in the etiological structure of which RA dominates. The most promising direction in this area is the use of artificial fluorophores, in particular quantum dots (QDs). The objective of this study was to evaluate the anti-infectious activity of the complex based on InP/ZnSe/ZnS 650 quantum dots and Tobramycin against Pseudomonas aeruginosa infection of the cornea. As an object of study, laboratory New Zealand rabbits (No. 6) were studied — 2 females, 4 males, which were induced bacterial keratitis by introducing a nosocomial Ps strain. aeruginosa in the structure of the cornea. The following antimicrobial agents were used: Tobramycin solution 5 ml for epibulbar application and a bioconjugate based on QD InP/ZnSe/ZnS 650 and tobramycin. Laboratory animals were divided into 2 groups. Rabbits of the 1st group, after the manifestation of the clinical picture of microbial keratitis, received instillations of tobramycin drops into the conjunctival sac every 2 hours for 3 days with a complete absence of positive clinical dynamics and a subsequent transition from day 4 in order to anatomically preserve the eyeball to instillations of the CT InP/ZnSe/ZnS complex 650 + Tobramycin. Rabbits of the 2nd group received instillations of the CT + Tobramycin complex and showed positive dynamics in relation to the regression of symptoms from the 2nd day of therapy. As methods of dynamic observation, photoregistration of the anterior segment with fluorescein staining and optical coherence tomography of the anterior segment were used. A clinical experiment has demonstrated the highest efficiency of the InP/ZnSe/ZnS 650 + Tobramycin complex in relation to Pseudomonas aeruginosa strain resistant to Tobramycin monotherapy.

Bacterial keratitis (BC) is a threatening condition for the anatomy and function of the eyeball and requires an immediate complex of therapeutic measures. Effective treatment that preserves the anatomical and functional result of the organ of vision, including various non-surgical and surgical methods, is the basis for the treatment of CD. Drug therapy includes, first of all, massive etiotropic therapy, which is usually represented by broad-spectrum antibiotics, antiseptics and anti-inflammatory drugs. These combinations make it possible to competitively influence all links of the pathological process, showing an additive effect. Promising non-surgical means in the fight against bacterial infection of the cornea, in particular with resistant microorganisms, is the use of Quantum dots, Mitomycin C, Matrix metalloproteinases. The most radical surgical methods of treatment are based on therapeutic keratoplasty, the purpose of which is to excise the infectious focus of the cornea and restore its transparency through transplantation of donor corneal tissue, but this method has a number of disadvantages and limitations in its implementation. Autoconjunctival keratoplasty is the oldest method of treatment of progressive corneal ulcers and this method should be considered rather as temporary or preparatory before through keratoplasty, due to the lack of visual functions. The least radical and relevant surgical methods of CD treatment today are the use of Corneal Crosslinking, Microdiathermocoagulation, Cyanoacrylate glue, Amniotic membrane transplantation. The expansion of the arsenal of methods of influencing the microbial process of the cornea and their further study will allow for a quick response in response to the rapidly developing antibiotic resistance in the world.