Синтез и противомикробная активность ацетанилидов и ацетилгидразонов тиетанилпиримидин-2,4(1&lt;I&gt;H&lt;/I&gt;,3&lt;I&gt;H&lt;/I&gt;)-дионового ряда

Мещерякова, С. А.; Катаев, Валерий Алексеевич; Фаттахова, Ильзира Ямилевна; Николаева, К. В.; Булгаков, А. К.

doi:10.30906/0023-1134-2015-49-9-28-31

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“…6-метил-3-(тиетан-3-ил)урацил синтезируют по методике, описанной в патенте Российской Федерации на изобретение RU 2485118 [8]. Известно, что 6-метил-3-(тиетан-3-ил)урацил стимулирует защитную активность фагоцитов, обладает противомикробной активностью [9]. Эпителий роговицы вырабатывает собственный экстрацеллюлярный матрикс, который прикрепляется к нижележащему слою Боумена и обеспечивает структурную поддержку, регулирует с помощью различных рецепторов эпителиальную миграцию, пролиферацию, дифференцировку, адгезию и апоптоз [10].…”

Section: результаты и обсуждениеunclassified

New Drugs for Ophthalmology Based on 6-methyl-3-(thietan-3-yl)uracil (Experimental Research)

et al. 2021

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Purpose: develop of new drugs for ophthalmology based on 6-methyl-3-(thietan-3-yl)uracil and methyluracil.Materials and methods. An experimental study was carried out on 10 rabbits with a body weight of 3.5–4.0 kg of chinchilla breed. A thermal burn of the cornea in the eyes of 6 rabbits and a chemical burn of the cornea in the eyes of 4 rabbits were modeled. Therapy with the use of drugs was carried out: ophthalmic ointment — in thermal burns, ophthalmic medicinal films based on 6-methyl-3-(thietan-3-yl)uracil and methyluracil in chemical burns.Results. The use of ophthalmic ointment based on 6-methyl-3-(thietan-3-yl)uracil for thermal burns led to a decrease in conjunctival hyperemia and resorption of corneal edema by 4–5 days. On the 14th day of therapy, the microscopic picture of the rabbits cornea had the usual normal structure. The use of 6-methyl-3-(thietan-3-yl)uracil and methyluracil based ophthalmic drug films yielded the following results: centripetal epithelialization of corneal erosion was observed, epithelial regeneration was higher with the use of methyluracil eye drug films and total epithelization was achieved on the 7th day of observation than when using eye drug films based on 6-methyl-3-(thietan-3-yl)uracil, where total epithelization occurred on the 14th day. Complete restoration of the surface epithelial layer of the cornea in both groups was observed on the 21st day.Conclusions. The use of new drugs based on 6-methyl-3-(thietan-3-yl)uracil and methyluracil in various types of corneal burns showed good tolerance in the eyes of experimental animals, shortened the treatment time, and achieved high wound healing efficacy.

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Section: результаты и обсуждениеunclassified

New Drugs for Ophthalmology Based on 6-methyl-3-(thietan-3-yl)uracil (Experimental Research)

et al. 2021

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Effect of ophthalmic drug films with methyluracil and 6-methyl-3-(thietan-3-yl)uracil on the thickness of the corneal epithelium

Габдрахманова

Курбанов

2021

Ophthalmology Reports

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BACKGROUND: Development and testing of drugs with regenerative and anti-inflammatory properties. It is advisable using them in keratopathy development and impairments of trophic processes, at the action of preservatives against the background of long-term local IOP-lowering therapy for glaucoma, as well as in the presence of a surgical wound in the area of the procedure, the last causing discomfort in many patients, foreign body sensation, and ocular irritation during the postoperative period in glaucoma treatment. AIM: To evaluate the effect of ophthalmic drug films (ODF) with 6-methyl-3- (thietan-3-yl)uracil and methyluracil on the thickness of the corneal epithelium after experimental chemical burn. MATERIALS AND METHODS: A histomorphological analysis of the cornea of 17 rabbits (34 eyes) of the Chinchilla breed after experimental chemical burn was carried out, the wound healing and keratoprotective properties of ophthalmic drug films were evaluated. Ophthalmic drug films with 6-methyl-3-(thietan-3-yl)uracil were placed in right eyes of 15 rabbits, and those with methyluracil were placed in left eyes of same rabbits. Two rabbits (4 eyes) served as control: their right eyes were left without wound healing therapy, while left eyes received dexpanthenol 5% gel (Corneregel) 4 times a day. The animals were followed-up for 21 days, morphological changes in the cornea were assessed on the 2nd, 7th, 14th and 21st days of the study. RESULTS: Different results were obtained depending on the ODF used. The use of ODF with methyluracil on days 27 led to an increase in the thickness and the number of epithelial layers compared to ophthalmic drug films with 6-methyl-3-(thietan-3-yl)uracil, where epithelial reactivity was observed by 14 days. On the 21st day of follow-up, the microscopic picture of the cornea in the right and the left eyes was characterized by total restoration and healing of the corneal epithelium. CONCLUSIONS: Ophthalmic drug films therapy with methyluracil and 6-methyl-3-(thietan-3-yl)uracil leads to histologically correct and rapid epithelialization of the cornea after a chemical burn.

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Comparative Evaluation of the Reparative Effect of Eye Ophthalmic Drug Films With Methyluracil After Surgical Treatment of Glaucoma (Experimental Research)

Курбанов,

Габдрахманова,

Курбанова

2023

Scientific Researches in the Kyrgyz Republic

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Актуальность. Длительное гипотензивное лечение, предшествующее хирургическому лечению за счет негативного влияния консервантов, входящих в состав местных гипотензивных лекарств, инволютивные изменения органа зрения, наличие сахарного диабета при первичной открытоугольной глаукоме сопровождаются нарушением гемомикроциркуляции и гидродинамики. Вышеизложенное может привести к развитию дистрофических изменений тканей глаза с формированием атрофической (тонкой, слабой) конъюнктивы. При наложении непрерывного шва появляются перфорации, через которые происходит наружная фильтрация, существенно снижающая эффективность хирургического лечения первичной открытоугольной глаукомы, что определяет актуальность поиска новых эффективных лекарственных препаратов. Цель работы – сравнительная оценка репаративного эффекта глазных лекарственных пленок c метилурацилом после лимбэктомии в эксперименте. Проведенные гистоморфологические исследования доказали ГЛП с метилурацилом положительно влияет на процесс регенерации послеоперационной раны и не приводит к избыточному рубцеванию. Abstract: Long-term antihypertensive treatment prior to surgical treatment due to the negative effect of preservatives included in local antihypertensive drugs, involutive changes in the organ of vision, the presence of diabetes mellitus in primary open-angle glaucoma are accompanied by impaired hemomicrocirculation and hydrodynamics. The foregoing can lead to the development of dystrophic changes in the tissues of the eye with the formation of an atrophic (thin, weak) conjunctiva. When a continuous suture is applied, perforations appear through which external filtration occurs, which significantly reduces the effectiveness of surgical treatment of primary open-angle glaucoma, which determines the relevance of the search for new effective drugs. The aim of the work is a comparative assessment of the reparative effect of ophthalmic drug films (ODF) with methyluracil after limbectomy in the experiment. The conducted histomorphological studies have proved ODF with methyluracil positively affects the process of postoperative wound regeneration and does not lead to excessive scarring. Актуалдуулугу. Антигипертензиялык препараттардын курамына кирген консерванттардын узак мөөнөттүү колдонуу глаукоманын хирургиялык дарылоо алдындагы терс таасиринен, көрүү органынын инволютивдик өзгөрүүлөрүнөн, кант диабетинин болушунан улам ачык бурчтуу глаукомада гемикроциркуляциянын жана гидродинамикасынын бузулушу менен коштолот. Жогоруда айтылгандар атрофиялык (ичке, алсыз) конъюнктиванын пайда болушу менен көздүн ткандарында дистрофиялык өзгөрүүлөрдүн өнүгүшүнө алып келиши мүмкүн. Үзгүлтүксүз тиккен кезде перфорациялар пайда болот, алар аркылуу тышкы фильтрация пайда болот, бул биринчилик ачык бурчтуу глаукоманы хирургиялык дарылоонун натыйжалуулугун олуттуу төмөндөтөт, бул жаңы эффективдүү дарыларды издөөнүн актуалдуулугун аныктайт. Иштин максаты – экспериментте лимбектомиядан кийин метилурацил менен көз дарылык пленкалардын репаративдик таасирин салыштырып баалоо. Жүргүзүлгөн гистоморфологиялык изилдөөлөр метилурацил менен көз дарылык пленкаларын операциядан кийинки жараатты калыбына келтирүү процессине оң таасирин тийгизип, ашыкча тырыктарга алып келбей турганын далилдеди.

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Синтез и противомикробная активность ацетанилидов и ацетилгидразонов тиетанилпиримидин-2,4(1<I>H</I>,3<I>H</I>)-дионового ряда

Cited by 3 publications

References 0 publications

New Drugs for Ophthalmology Based on 6-methyl-3-(thietan-3-yl)uracil (Experimental Research)

New Drugs for Ophthalmology Based on 6-methyl-3-(thietan-3-yl)uracil (Experimental Research)

Effect of ophthalmic drug films with methyluracil and 6-methyl-3-(thietan-3-yl)uracil on the thickness of the corneal epithelium

Comparative Evaluation of the Reparative Effect of Eye Ophthalmic Drug Films With Methyluracil After Surgical Treatment of Glaucoma (Experimental Research)

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