scholarly journals Directed synthesis and search of pharmaceutical substances with hypoglycemic activity in the series of 4-aryl-2-hydroxy-4-oxo-2-butenoic acids

2011 ◽  
Vol 10 (5) ◽  
pp. 86-90
Author(s):  
N. A. Pulina ◽  
A. I. Krasnova ◽  
F. V. Sobin ◽  
T. A. Yushkova ◽  
V. V. Yushkov
Keyword(s):  
Bromine Atom ◽  
Hypoglycemic Activity ◽  
Reference Drug ◽  
Highly Active ◽  
Pharmaceutical Substances ◽  
Directed Synthesis ◽  
Low Toxic ◽  
Heterocyclic Moiety ◽  
Active Substances

The paper deals with directed synthesis and study of hypoglycemic activity of N-heterylamides of 4-aryl-2-hydroxy-4-oxo-2- butenoic and 4-aryl-3-bromo-2, 4-dioxobutanoic acids. Hypoglycemic activity of 28 compounds was under research. Some regularities of the influence of the heterocyclic moiety structure and the bromine atom on the activity of the compounds were obtained. Two low-toxic and highly active substances comparable in potency with the reference drug were identified.

scholarly journals Synthesis, antimicrobial and anti-cancer activities of some new N-ethyl, N-benzyl and N-benzoyl-3-indolyl heterocycles

2012 ◽  
Vol 62 (2) ◽  
pp. 157-179 ◽  
Author(s):  
Eslam El-Sawy ◽  
Adel Mandour ◽  
Khaled Mahmoud ◽  
Inas Islam ◽  
Heba Abo-Salem
Keyword(s):  
Hydrazine Hydrate ◽  
Hydroxylamine Hydrochloride ◽  
Reference Drug ◽  
Highly Active ◽  
Anti Cancer ◽  
Hct 116 ◽  
New Compounds ◽  
Substituted 1 ◽  
Isoxazole Derivatives

Synthesis, antimicrobial and anti-cancer activities of some newN-ethyl,N-benzyl andN-benzoyl-3-indolyl heterocyclesA series of 1-(N-substituted-1H-indol-3-yl)-3-arylprop-2-ene-1-ones (2a, b-4a, b) were prepared and allowed to react with urea, thiourea or guanidine to give pyrimidine derivatives5a, b-13a, b. Reaction of2a, b-4a, bwith ethyl acetoacetate in the presence of a base gave cyclohexanone derivatives14a, b-16a, b. Reaction of the latter compounds with hydrazine hydrate afforded indazole derivatives17a, b-19a, b. On the other hand, reaction of2a, b-4a, bwith some hydrazine derivatives, namely hydrazine hydrate, acetyl hydrazine, phenylhydrazine and benzylhydrazine hydrochloride, led to the formation of pyrazole derivatives20a, b-31a, b. Moreover, reaction of2a, b-4a, bwith hydroxylamine hydrochloride gave isoxazole derivatives32a, b-34a, b. The newly synthesized compounds were tested for their antimicrobial activity and showed that 4-(N-ethyl-1H-indol-3-yl)-6-(p-chlorophenyl)-pyrimidine-2-amine (11b) was the most active of all the test compounds towardsCandida albicanscompared to the reference drug cycloheximide. Eighteen new compounds, namely pyrimidin-2(1H)-ones5a, b-7a, b, pyrimidin-2(1H)-thiones8a, b-10a, band pyrimidin-2-amines11a, b-13a, bderivatives, were tested for theirin vitroantiproliferative activity against HEPG2, MCF7 and HCT-116 cancer cell lines. 4-(N-ethyl-1H-indol-3-yl)-6-(p-methoxyphenyl)-pyrimidin-2-amine (11a)was found to be highly active withIC50of 0.7 μmol L-1.

scholarly journals DEUTERIUM AS A TOOL FOR CHANGING THE PROPERTIES OF PHARMACEUTICAL SUBSTANCES (REVIEW)

2021 ◽  
pp. 65-73
Author(s):  
ANTON V. SYROESHKIN ◽  
TATYANA V. PLETENEVA ◽  
ELENA V. USPENSKAYA ◽  
OLGA V. LEVITSKAYA ◽  
IRINA V. TARABRINA ◽  
...  
Keyword(s):  
Rapid Development ◽  
Essential Elements ◽  
Pharmaceutical Ingredients ◽  
Kinetic Isotope ◽  
Pharmaceutical Substances ◽  
Essential Trace Elements ◽  
Reduced Toxicity ◽  
New Compounds ◽  
First Time ◽  
Active Substances

The review is devoted to the influence of the hydrogen isotope–deuterium on biological models of organisms and the biological activity of pharmaceutical substances. The positions of the influence of deuterium on the properties of active pharmaceutical ingredients and excipients are examined from different perspectives. The first position reflects an increase in the kinetic isotope effect (KIE) in processes involving known pharmaceutical substances in aqueous solutions with a deuterium/protium ratio (D/H) below natural. For the first time, the dose-response diagram shows the identity of deuterium with essential trace elements, when a deficiency and excess of an element reduces the organism's vitality. Improved kinetic characteristics are demonstrated for the molecular and organism levels of different hierarchical gradations. In particular, they consist in the possibility of increasing the dissolution rate of substances by influencing the carbohydrate mutarotation processes and the optical activity of chiral substances, increased accumulation of essential elements in medicinal plants and other processes associated with a possible change in metabolic pathways in the cell and the organism as a whole. The second considered position of the influence of deuterium is associated with the use of deuterated substances–new compounds or obtained by substitution of protium in known protium analogues. The KIE is presented, which is expressed in a decrease in the biotransformation rate as a result of deuteration, it allows predicting a rapid development of the new direction in the development of drugs. Having an identical therapeutic effect, deuterated analogs provide improved pharmacokinetic characteristics, such as reduced toxicity, blocked epimerization of optically active substances, and a change in the mechanisms of biotransformation. The obtained results make it possible to predict the mechanisms of the effect of deuterium on the biochemical transformations of pharmaceutical substances in the organism.

scholarly journals Members of the family Lamiaceae Lindl. as sources of medicinal plant raw materials to obtain neurotropic drugs

2020 ◽  
Vol 8 (1) ◽  
pp. 4-28
Author(s):  
Е. V. Zvezdina ◽  
J. V. Dayronas ◽  
I. I. Bochkareva ◽  
I. N. Zilfikarov ◽  
E. Yu. Babaeva ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
Scientific Literature ◽  
Raw Materials ◽  
Neurotropic Activity ◽  
Biologically Active ◽  
Plant Materials ◽  
Plant Raw Materials ◽  
Pharmaceutical Substances ◽  
The Family ◽  
Active Substances

The aim of this work is to review and analyze the data published in the modern scientific literature obtained in pharmacological, pharmacognostic and pharmacotechnological studies of various types of raw materials obtained from members of the family Lamiaceae L., which were sources of biologically active substances, pharmaceutical substances, total extracts and the drugs – with a neurotropic activity.Materials and methods. For the review, we used the information of scientific literature from open and accessible sources of the last twenty years, located in the scientific and technical libraries of institutions, as well as in electronic databases: Elibrary, PubMed, Scopus, Cyberleninka, GoogleAcademy, J-Stage. The search inquiries were: the species of the family Lamiaceae (Russian and Latin), the samples of medicinal plant materials based on them as well as the names of the drugs and biologically active substances obtained from these raw materials.Results. When working with the sources of scientific information, the main attention was paid to pharmacologic tests performed during the studies on laboratory animals and proving the presence of neurotropic activity in the studied objects – essential oils and extracts from plant raw materials: aqueous, aqueous alcoholic, and methanol ones. It has been established that the potential of the therapeutic and preventive application of pharmaceutical substances and drugs based on the medicinal plant materials obtained from 30 genera members of the Lamiaceae family, remains unrealized despite the close attention of various researchers.Conclusion. This review comprised 71 species from 30 genera. Despite the significant level of the previous study presented in the analysis of this publication, an enormous potential of this family’s species remains unexplored. In the future, they can be of both – pharmacognostic and practical interest, in particular, in creation of new medicinal preparations of the neurotropic action based on them.

scholarly journals In Vitro and In Vivo Studies of the Trypanocidal Effect of Novel Quinolines

2017 ◽  
Vol 62 (2) ◽  
Author(s):  
A. S. G. Nefertiti ◽  
M. M. Batista ◽  
P. B. Da Silva ◽  
D. G. J. Batista ◽  
C. F. Da Silva ◽  
...  
Keyword(s):  
Parasite Species ◽  
Oral Absorption ◽  
In Vivo Studies ◽  
Cure Rate ◽  
Reference Drug ◽  
Content Type ◽  
African Trypanosomes ◽  
Highly Active

ABSTRACT Therapies for human African trypanosomiasis and Chagas disease, caused by Trypanosoma brucei and Trypanosoma cruzi, respectively, are limited, providing minimal therapeutic options for the millions of individuals living in very poor communities. Here the effects of 10 novel quinolines are evaluated in silico and by phenotypic studies using in vitro and in vivo models. Absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties revealed that most molecules did not infringe on Lipinski's rules, which is a prediction of good oral absorption. These quinolines showed high probabilities of Caco2 permeability and human intestinal absorption and low probabilities of mutagenicity and of hERG1 inhibition. In vitro screens against bloodstream forms of T. cruzi demonstrated that all quinolines were more active than the reference drug (benznidazole [Bz]), except for DB2171 and DB2192, with five (DB2187, DB2131, DB2186, DB2191, and DB2217) displaying 50% effective concentrations (EC50s) of <3 μM (4-fold lower than that of Bz). Nine quinolines were more effective than Bz (2.7 μM) against amastigotes, showing EC50s ranging from 0.6 to 0.1 μM. All quinolines were also highly active in vitro against African trypanosomes, showing EC50s of ≤0.25 μM. The most potent and highly selective candidates for each parasite species were tested in in vivo models. Results for DB2186 were promising in mice with T. cruzi and T. brucei infections, reaching a 70% reduction of the parasitemia load for T. cruzi, and it cured 2 out of 4 mice infected with T. brucei. DB2217 was also active in vivo and cured all 4 mice (100% cure rate) with T. brucei infection.

Biologically Active Substances from Cacalia hastate Leaves. 1. Carbohydrates from Leaves and Their Hypoglycemic Activity

2004 ◽  
Vol 40 (1) ◽  
pp. 1-5 ◽  
Author(s):  
D. N. Olennikov ◽  
L. M. Tankhaeva ◽  
G. G. Nikolaeva ◽  
A. V. Tsyrenzhapov ◽  
S. M. Nikolaev ◽  
...  
Keyword(s):  
Hypoglycemic Activity ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Active Substances

scholarly journals The research of anti-inflammatory activity of 5-(5-bromofuran-2-yl)-4-ethyl-1,2,4-triazole-3-thion S-derivatives

2018 ◽  
pp. 78-82
Author(s):  
Ye. S. Pruglo
Keyword(s):  
Bromine Atom ◽  
Pharmacological Action ◽  
Inflammatory Activity ◽  
The Novel ◽  
Dimethylamino Group ◽  
Reference Drug ◽  
White Rats ◽  
Anti Inflammatory ◽  
Inflammatory Action

The studing of  anti-inflammatory activity of the novel compounds may give rise to the using of safer and more active drugs in the treatment of diseases which are shown NSAIDs. To further study the pharmacological properties of the synthesized c compounds were studied for acute toxicity and anti-inflammatory activity of 5-thio derivates of 3-(5-вromofuran-2-yl)-4-ethyl-(4H)-1,2,4-triazole at white rats by formalin method of acute edema. After investigation of anti-inflammatory activity in vivo of first synthesized 1,2,4-triazole derivatives it was found that potassium salt of 2-(4-ethyl-5-(5-bromfuran-2-yl)-1,2,4-triazoles 3-iltio) acetic acid (Compound 24) had the most significant anti-inflammatory activity. This compound suppressed the formation of edema quotes of rats at 59.87% and was more active than the reference drug diclofenac at 15.13%. There were established the patterns regarding chemical structure and pharmacological action of these substances. So replacing of bromine atom at the dimethylamino group in the para-position of the phenyl radical in the molecule of N'-(4-brombenzyliden)-2-((5-(5-bromfuran-2-yl)-4-ethyl-4H-1,2,4-triazole-3-yl)tio)acetic hydrazid (Compound 36) was accompanied by appearence of the anti-inflammatory action. It was revealed that in the number from the ammonium salt (Compound 30) to monoethanolamonium salt (Compound 23) and to the morpholinum salt (Compound 22) it was observed an increase of inflammation and probably growing number of pro-inflammatory mediators released.

Central Monoamine Neurons

1973 ◽  
Vol 31 ◽  
pp. 528-529
Author(s):  
T. Hökfelt
Keyword(s):  
Brain Function ◽  
Physiological Role ◽  
Neuronal Cell ◽  
Electron Microscopic Level ◽  
Electron Microscopic ◽  
Biogenic Monoamines ◽  
Highly Active ◽  
Monoamine Neurons ◽  
Central Monoamine ◽  
Active Substances

Considerable interest has been focused on a group of biologically highly active substances often called biogenic monoamines including dopamine (DA), noradrenaline (NA), adrenaline (A) and 5-hydroxytryptamine (5-HT). Initially their existence in various non-neuronal cell systems and their role as hormones called for extensive research efforts. Subsequently their possible involvement in neurotransmission both in the peripheral and central nervous system has been studied in laboratories all over the world.Today a wide variety of methods are available for studies on monoamine neurons among others histochemical techniques at the light and electron microscopic level. These techniques have been of importance not only for identification and mapping of such neurons but also for the understanding of their physiological role(s) e.g. in brain function.

EDTA-Directed Synthesis of Highly Active Porous Titania with Bicrystalline Framework

2007 ◽  
Vol 7 (12) ◽  
pp. 4339-4345 ◽  
Author(s):  
Yun Liu ◽  
Chun-Yan Liu ◽  
Zhi-Ying Zhang
Keyword(s):  
Organic Molecules ◽  
High Surface ◽  
Hydrothermal Process ◽  
High Surface Area ◽  
Porous Structures ◽  
Sodium Salts ◽  
Highly Active ◽  
Porous Titania ◽  
Directed Synthesis ◽  
Facile Hydrothermal Process

Porous titania with bicrystalline (anatase and rutile) framework was successfully synthesized by a facile hydrothermal process using inexpensive and nontoxic organic molecules, EDTA (ethylenediamine-tetra-acetic acid) or its sodium salts as a template, which could be removed from porous titania by the extraction with sodium hydroxide aqueous solution and then easily recovered by acidification. XRD investigation suggested that the ratio of anatase to rutile could be readily tuned by employing different sodium salts of EDTA. All of as-prepared porous titania showed higher activities than the commercial photocatalyst P25 for the degradation of methyl orange (MO), because of the high surface area, bicrystalline phase composition and bimodal porous structures.

scholarly journals Study of hypoglycemic activity of tablets of “Gliphasonorm” capsules and “Gliphasolin” on the model of streptozotocin-induced diabetes in rats

2015 ◽  
Vol 17 (3) ◽  
Author(s):  
V. A. Rybak ◽  
L. M. Maloshtan
Keyword(s):  
Experimental Model ◽  
Marked Reduction ◽  
Glycosylated Hemoglobin ◽  
Diabetes Type 2 ◽  
Diabetic Control ◽  
Diabetes Type ◽  
Hypoglycemic Activity ◽  
Reference Drug ◽  
Streptozotocin Induced Diabetes

<p>The conducted research allowed to determine that the tablets “Gliphasonorm” capsules and “Gliphasolin” in an<br />experimental model of streptozotocin-induced diabetes significantly reduced the level of glycosylated hemoglobin,<br />decreased with the level of glucose in the blood of animals compared to diabetic control. After 14 days of the study<br />capsules “Gliphasolin” showed a more pronounced hypoglycemic activity (4.4 % and 8.0 % greater) than tablets<br />“Gliphasonorm” and the reference drug metformin. Under the action caps “Gliphasolin” on the 12th day of the study<br />showed marked reduction of glycosylated hemoglobin in the blood of animals (3.1 % and 5.6 % greater) than that of<br />the tablets of “Gliphasonorm” and metformin. Capsules “Gliphasolin” and tablets “Gliphasonorm” based bioflavonoid<br />complex from beans are promising in the therapy of diabetes type 2 on the background of obesity and reduce the<br />risk of micro- and macroangiopathies.</p>

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