Pharmacological Activity of a Pyrimidine Derivatives

Osipov, A. O.; Пурыгин, П. П.; Дубищев, А. В.; Osipova, A. A.

doi:10.18287/2541-7525-2011-17-8-167-172

Cited by 4 publications

(3 citation statements)

References 3 publications

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“…The statistical data provide reliable evidence of an increasing rate of natural disasters and of the associated losses over time. This tendency is frequently viewed as resulting from increasing population, urbanization, a growing number of hazardous facilities, and a general deterioration of the geo ecologic environment [3,4]. This interpretation is not however entirely correct.…”

Section: Short Communicationmentioning

confidence: 99%

Dependence of Losses from Natural Hazards on the Prosperity of Societies: A Brief Review

Родкин

2020

JAAS

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Section: Short Communicationmentioning

confidence: 99%

Dependence of Losses from Natural Hazards on the Prosperity of Societies: A Brief Review

Родкин

2020

JAAS

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“…Pyrimidinylpiperazines are also used in medicine, for example 1-(2-pyrimidinyl)piperazine is an active metabolite of buspironanxiolytic medicine (tranquilizer), which also has an antidepressant effect [28,30]. In addition, many other drugs have a pyrimidine fragment in their structure: acyclovir (an antiherpetic drug), methyluracil (a regeneration stimulant), trimethoprim (a dihydrofolate reductase inhibitor of bacteria), chloridine (an antimalarial agent), risperidone (an antipsychotic agent), vitamin B1; cytosine, thymine, uracil, which are widely known and are part of nucleotides as well they have a pyrimidine nucleus [46]. The objective of this work was the synthesis of new piperazine derivatives and the study of their general toxicity, local anaesthetic activity and the relationship with the chemical structure.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

KHAIITOVA¹

2023

FARMACIA

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N-substituted piperazines, an important class of compounds with different pharmacological activities were taken as the basic starting object for the synthesis and study of α-aminophosphonates. The objective of the study was the synthesis, analysis of biological effects (toxicity and local anaesthetic activity) of some new piperazine derivatives, and the evaluation of their potential pharmacological effects. The new piperazine derivatives were coded as LAS-276, LAS-277, LAS-278, where LAS is a local anaesthetic substance. The compounds were synthesized under the conditions of the Kabachnik-Fields reaction. Their acute toxicity in mice, the local anaesthetic activity in a regional and infiltration anaesthesia models were studied, and their estimated pharmacological activity was analysed using the online PASS (Prediction of Activity Spectra for Substances) program. In a series of experiments the administration of high doses of the studied compounds has not caused death of laboratory animals. The study of local anaesthetic activity in the infiltration anaesthesia model showed varying degrees of activity. The compounds showed moderate activity on the regional anaesthesia model. The PASS analysis revealed a very high probability of thrombolytic, anticoagulant, antisclerotic effects and stimulation of endothelin receptors. The implemented studies revealed the low toxicity, moderate local anaesthetic activity of the studied piperazine compounds. There is also a high probability of their thrombolytic activity, which requires further research. RezumatPiperazinele N-substituite sunt o clasă importantă de compuși cu activitate farmacologică ce stau la baza sintezei și studiul αaminofosfonaților. Obiectivele studiului au fost sinteza, analiza efectelor biologice (toxicitate și activitate anestezică locală) și evaluarea efectelor farmacologice ale noilor derivați de piperazină. Compușii au fost sintetizați în condițiile reacției Kabachnik-Fields. Apoi s-a studiat toxicitatea lor după administrarea în doză unică la șoareci, activitatea anestezică locală într-o anestezie regională și modele de infiltrație. Activitatea lor farmacologică a fost evaluată folosind programul online PASS (Predicția Spectrelor de Activitate pentru Substanțe). Într-o serie de experimente, administrarea de doze mari din compușii studiați nu a provocat moartea animalelor de laborator. Studiul activității anestezice locale în modelul de anestezie prin infiltrare a arătat grade variate de activitate. Compușii au prezentat activitate moderată în modelul de anestezie regională. Analiza PASS a relevat o probabilitate foarte mare de efecte trombolitice, anticoagulante, antisclerotice și de stimulare a receptorilor de endotelină. Studiile implementate au evidențiat toxicitatea scăzută, precum și activitatea anestezică locală moderată a compușilor piperazinici studiați. Există, de asemenea, o probabilitate mare a activității lor trombolitice, ceea ce necesită cercetări suplimentare.

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“…At the same time, ejection systems have low efficiency and therefore are used when other solutions are not possible. In the studies [10][11], a description and study of exhaust ventilation systems is given, where ejector installations have been used that work reliably, regardless of the volume of released flammable, explosive, and abrasive impurities.…”

Section: Introductionmentioning

confidence: 99%

A study of flow characteristics in a low-pressure ejector installation

2021

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Production processes sometimes are accompanied by the release of hazardous substances, the composition and volume of which is determined by the production technology. When designing ventilation systems for paint departments, special attention is paid to safety concerns, since all paint coatings are corrosive and flammable substances. Besides, solvent vapors are explosive. For local ventilation of painting chambers, it is rational to use safe exhaust systems with an ejector, which works sturdily, regardless of the release of flammable and explosive impurities. The ejector is simple in design and can operate in a wide range of changes in the parameters of the state of airflow. The model of the ejection unit is synthesized using the universal modeling package ChemCad, which contains a highly developed database of airflow parameters, which allows for solving various applied problems. Numerical modeling was carried out using the software package - FLUENT. In work, a calculation was carried out and a low-pressure ejector was designed for a typical painting booth. The calculation results are presented in the form of graphs and tables of pressures, velocities, flow rates in characteristic sections, pressure losses in the sections of the ejector installation.The ejection coefficient was also calculated.

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Pharmacological Activity of a Pyrimidine Derivatives

Cited by 4 publications

References 3 publications

Dependence of Losses from Natural Hazards on the Prosperity of Societies: A Brief Review

Dependence of Losses from Natural Hazards on the Prosperity of Societies: A Brief Review

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

A study of flow characteristics in a low-pressure ejector installation

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