Електронний архів Національного фармацевтичного університету
Not a member yet
13799 research outputs found
Sort by
Synthesis of the 6-(1H-benzimidazol-2-yl)-3,5-dimethyl-2- oxo(thioxo)-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-ones with potent biological activity
No full textДоказательство региоселективности протекания циклизации 1-этил-3-[4-6,7,8,9-тетрагидро-5Н-[1,2,4]триазоло[4,3-а]азепин-3-ил)фенил]тиомочевины с α-бромкетоном
No full textAn important step in the creation of potential drugs is to confirm the structure of the synthesized compounds. This requires the use of modern physical and physicochemical methods. Nowadays a perspective scientific direction for searching biologically active substances is the study of 2-R-imino-1,3-thiazoline derivatives.
The purpose of the present work is to study a regioselectivity of cyclization of 1-ethyl-3-[4-(6,7,8,9-tetrahydro-5Н-[1,2,4]triazolo[4,3-а]azepin-3-yl)phenyl]thiourea reaction with 2-bromo-1-phenylethanone.
Results and discussion. The structure of the interaction product was determined by the methods 1H NMR spectroscopy and X-ray analysis. Activating energy of tautomer 1A belower than 1B one, the state of 1B has modest lower relative energy, consequently tautomer 1A is more credible state. So we can make the conclusion that the reaction will go by the way 1-1A-3A.
Experimental part. Quantum-chemical calculations of electronic structure, geometry and thermodynamics parameters of initial thiourea three tautomers were calculated with the density functional theory (DFT) methods using the GAUSSIAN W09 computer program. The effect of the solvent was considered out within the framework of polarized continuum model (PCM).
Conclusions. Based on the physico-chemical studies and quantum chemical calculations of the reaction cyclization direction the conclusion has been made that the cyclization reaction of 1-ethyl-3-[4-(6,7,8,9-tetrahydro-5Н-[1,2,4]triazolo[4,3-а]azepin-3-yl)phenyl]thiourea 1 with 2-bromo-1-phenylethanone 2 is regioselective and leads to formation of more thermodynamically advantageous isomer 3A
Experience of the use of L-arginin in complex with betain in treatment of erectile dysfunction
No full textПоказан позитивный опыт использования препарата Бетаргин, в состав которого входят L-аргинин и
бетаин, при лечении эректильной дисфункции у 26 мужчин с избыточной массой тела, гипертонической
болезнью и гиперхолестеринемией. В случаях применения препарата отмечается полная нормализация
эректильной функции у 30,8% больных на фоне снижения уровней печеночных трансаминаз, холестерина
и гомоцистеина в крови и увеличения величин тестостерон-эстрадиолового соотношения.Shown the positive experience of using the drug Betargin, which is composed of L-arginine and betaine in
the treatment of erectile dysfunction in 26 men with overweight, hypertension and hypercholesterolemia. In cases
where the drug showed a complete normalization of erectile function in 30.8% of patients on the background of
reducing levels of hepatic transaminases, cholesterol and homocysteine in the blood and increase quantities of
testosterone-estradiol ratio
Аналіз асортименту екстемпоральних лікарських засобів, які випускаються аптеками м. Харкова та Харківської області
No full textАнализ и технология экстемпоральной рецептуры для фармакотерапии сердечно-сосудистых заболеваний
No full textПроанализирована номенклатура экстемпоральных прописей для лечения сердечно-сосудистых заболеваний. Лекарственные препараты в аптеках изготавливают в форме порошков, растворов, настоев и отваров, капель и др. Приведены особенности технологии основных экстемпоральных прописей. Показана возможность их использования в качестве альтернативных препаратов готовым лекарственным средствам для фармакотерапии этих заболеваний.The nomenclature of extemporal prescriptions for the treatment of cardiovascular diseases was analyzed. Medicines in pharmacies are made in the form of powders, solutions, infusions and decoctions, drops, etc. Technological features of the basic extemporal prescriptions are given. The possibility of their use as alternative drugs for ready-made medicines for the pharmacotherapy of these diseases is shown
Synthesis and in silico research of derivatives of 3-allyl-4-(R-phenyl)-N-(R1-phenyl)thiazole-2-imine
Get PDFThe synthesis of those new derivatives of 3-allyl-4-(R-phenyl)-N-(R1-phenyl)-thiazole-2-imine was conducted which consist substituted aromatic radicals. Structure of the compounds synthesized has proved by means of a comprehensive use of modern physical and chemical methods of analysis. In silico research has been conducted of the potential molecular mechanisms of cardioprotective action of the obtained substances with the method of a soft molecular docking, and recommendations to the rational design of the ligands have been mad
