Biologically Active, Water-soluble Derivatives of Nystatin – Chemical Studies

Chemotherapy ◽  
1963 ◽  
Vol 6 (6) ◽  
pp. 326-343 ◽  
Author(s):  
G. Rapi ◽  
P. Cocchi ◽  
E. Belgodere
Keyword(s):  
Water Soluble ◽  
Biologically Active ◽  
Chemical Studies ◽  
Derivatives Of

scholarly journals Quantum-Chemical Search for Keto Tautomers of Azulenols in Vacuo and Aqueous Solution

Symmetry ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 497
Author(s):  
Ewa D. Raczyńska
Keyword(s):  
Aqueous Solution ◽  
Quantum Chemical ◽  
Biologically Active ◽  
Deprotonation Reaction ◽  
Chemical Studies ◽  
Quantum Chemical Studies ◽  
Scanty Information ◽  
Derivatives Of ◽  
Common Anion ◽  
Tautomeric Mixture

Keto-enol prototropic conversions for carbonyl compounds and phenols have been extensively studied, and many interesting review articles and even books appeared in the last 50 years. Quite a different situation takes place for derivatives of biologically active azulene, for which only scanty information on this phenomenon can be found in the literature. In this work, quantum-chemical studies have been undertaken for symmetrically and unsymmetrically substituted azulenols (constitutional isomers of naphthols). Stabilities of two enol (OH) rotamers and all possible keto (CH) tautomers have been analyzed in the gas phase {DFT(B3LYP)/6-311+G(d,p)} and also in aqueous solution {PCM(water)//DFT(B3LYP)/6-311+G(d,p)}. Contrary to naphthols, for which the keto forms can be neglected, at least one keto isomer (C1H, C2H, and/or C3H) contributes significantly to the tautomeric mixture of each azulenol to a higher degree in vacuo (non-polar environment) than in water (polar amphoteric solvent). The highest amounts of the CH forms have been found for 2- and 5-hydroxyazulenes, and the smallest ones for 1- and 6-hydroxy derivatives. The keto tautomer(s), together with the enol rotamers, can also participate in deprotonation reaction leading to a common anion and influence its acid-base properties. The strongest acidity in vacuo exhibits 6-hydroxyazulene, and the weakest one displays 1-hydroxyazulene, but all azulenols are stronger acids than phenol and naphthols. Bond length alternation in all DFT-optimized structures has been measured using the harmonic oscillator model of electron delocalization (HOMED) index. Generally, the HOMED values decrease for the keto tautomers, particularly for the ring containing the labile proton. Even for the keto tautomers possessing energetic parameters close to those of the enol isomers, the HOMED indices are low. However, some kind of parallelism exists for the keto forms between their relative energies and HOMEDs estimated for the entire molecules.

FULLERENECARBOXYLIC ACIDS AND PROSPECTS FOR THEIR USE IN THE CHEMISTRY OF DRUGS

2018 ◽  
Vol 18 (2) ◽  
pp. 19-28
Author(s):  
E V Litasova ◽  
L B Piotrovskiy
Keyword(s):  
Delivery Systems ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Carboxyl Groups ◽  
Derivatives Of ◽  
Active Substances

Among the various derivatives of fullerenes, compounds containing carboxyl groups (carboxyfullerenes) occupy a prominent place. The reason is that the introduction of carboxyl groups makes it possible to obtain water-soluble derivatives of highly lipophilic fullerenes. The review deals with matters of synthesis and structure of carboxyfullerenes, the influence of the amount and structure of the addends on the solubility of the entire compound, various aspects of the usage of these compounds as independent biologically active substances and carriers for creation of various delivery systems.

scholarly journals Natural Sesquiterpene Lactones as Renewable Chemical Materials for New Medicinal Products

2013 ◽  
Vol 15 (3) ◽  
pp. 163 ◽  
Author(s):  
S.M. Adekenov
Keyword(s):  
Chemical Modification ◽  
Sesquiterpene Lactones ◽  
Physiological Activity ◽  
Chemical Properties ◽  
Water Soluble ◽  
Biologically Active ◽  
Isolation And Purification ◽  
Environmentally Safe ◽  
Renewable Material ◽  
Derivatives Of

<p>Literature data and own research results on the technology for isolating natural sesquiterpene lactones such as arglabin, alantolactone, artemisinin, grosheimin, isoalantolactone, parthenolide, santonin and potential possibilities of their use as renewable material for obtaining new compounds as well as biologically active derivatives are generalized in this review. Sesquiterpene lactones from plants are promising sources for the development and practical application of new original medical products possessing antitumor, anti-inflammatory, antimalarial, antiulcer, antiviral and immune-stimulating action. The technology for isolating sesquiterpene lactones is based on the extraction of raw plant material by different organic solvents with the subsequent chromatographic purification. The effective and environmentally safe technology for isolation and purification of sesquiterpene lactone arglabin from <em>Artemisia glabella</em> Kar. et Kir. by the СО<sub>2</sub>-extraction method is developed. Thereat, it was experimentally determined that the method for isolating arglabin from CO<sub>2</sub> extract of <em>Artemisia glabella</em> Kar. et Kir. using centrifugal partition chromatography is effective for preparative isolation of the active substance and its manufacturing application. It is practically important to obtain water-soluble derivatives of biologically active sesquiterpene lactones and also to use the nanotechnology achievements for directed transportation of a molecule of the medicine in the human body thereby reducing toxicity of an active component. Promising direction is chemical modification of molecules in sesquiterpene lactones which are renewable material for obtaining new derivatives, thanks to which it becomes possible to solve two problems at the same time. Firstly, these researches help to obtain derivatives with higher biological activity or improved physical and chemical properties. Secondly, these researches enable us to disclose the mechanism of action of different medicines within the framework of “structure-activity” correlation. The article presents the literature data and own results on chemical modification of sesquiterpene lactones of alantolactone, arglabin, artemisinin, grosheimin, isoalantolactone, parthenolide and santonin. Various reactions on functional groups of these molecules were used to obtain a number of new derivatives of sesquiterpene lactones containing haloid-, pyrazole-, triazole-, amino-, dialkylamino-, hydroxy-, dialkyl phosphonate- and cyclopropane groups, which have shown high physiological activity.</p>

The content of decenoic acids in drone brood preparations and combined preparations based on it

Biomics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 389-393
Author(s):  
D.V. Mitrofanov ◽  
N.V. Budnikova
Keyword(s):  
Royal Jelly ◽  
Storage Conditions ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Strict Adherence ◽  
Drone Brood ◽  
Wide Range ◽  
Active Substances ◽  
Melanin Complex

The drone brood contains a large number of substances with antioxidant activity. These substances require stabilization and strict adherence to storage conditions. Among these substances are unique decenoic acids, the content of which is an indicator of the quality of drone brood and products based on it. The ability of drone brood to reduce the manifestations of oxidative stress is shown. There are dietary supplements for food and drugs based on drone brood, which are used for a wide range of diseases. Together with drone brood, chitosan-containing products, propolis, royal jelly can be used. They enrich the composition with their own biologically active substances and affect the preservation of the biologically active substances of the drone brood. Promising are the products containing, in addition to the drone brood, a chitin-chitosan-melanin complex from bees, propolis, royal jelly. The chitin-chitosan-melanin complex in the amount of 5% in the composition of the adsorbent practically does not affect the preservation of decenic acids, while in the amount of 2% and 10% it somewhat worsens. The acid-soluble and water-soluble chitosan of marine crustaceans significantly worsens the preservation of decenoic acids in the product. Drone brood with royal jelly demonstrates a rather high content of decenoic acids. When propolis is introduced into the composition of the product, the content of decenoic acids increases according to the content of propolis.

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

On the diagnostics of Adonis L. species (Ranunculaceae) of the Russian flora

2020 ◽  
pp. 3-14
Author(s):  
Aleksandr Luferov
Keyword(s):  
Raw Materials ◽  
Natural Populations ◽  
Structural Features ◽  
Biologically Active ◽  
Scientific Medicine ◽  
Diagnostic Features ◽  
Plant Raw Materials ◽  
Similar Chemical ◽  
Chemical Studies ◽  
Alternative Sources

The article provides brief information about cardiotonic, sedative, cytostatic, diuretic, and antibacterial effects of biologically active compounds of Adonis L. (Ranunculaceae) species. Chemical studies allowed to identify the cardiac glycosides, or cardenolides: or cardenolides: adontoxin, adonitol, adonitoxigenin, acetyldigitoxin and others. In scientific medicine, it is currently allowed to use Adonis vernalis L. Other types of Adonis have a similar chemical composition and are offered as substitutes for this official species, for example, Adonis apennina L. Many Adonis species have limited natural resources, and in some regions are rare, requiring conservation of their natural populations. The search for alternative sources of medicinal plant raw materials, based on this, is relevant. The experimental part of our research was carried out using the morphological and geographical method with the involvement of information on ecology and phenology. For the first time summarizes the diagnostic features of Adonis flora of Russian flora. Previously unknown structural features (shape and size of anthers) were identified that characterize the subgenera Adonanthe and Adonis. Taxonomic study of the genus Adonis of the Russian flora allowed us to determine its species composition, clarify its systematic affiliation, and nomenclature synonyms. 9 species were identified. Of these, 6 are perennials belonging to the subgenus Adonanthe, section Consiligo, which includes 2 subsections: Amurenses (2 species) and Vernales, which is differentiated into 2 rows: Apenninae (2 species) and Vernales (2 species). Subgenus Adonis is represented by 2 sections: Adonis (1 species) and Lophocarpa with sections Aestivales (1 species) and Dentatae (1 species). For all the considered species and varieties, the main distribution areas are given. A key has been compiled to determine the wild Adonis species distributed in Russia.

Potential anticonvulsants: Substituted N-benzylidene derivatives of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins

1983 ◽  
Vol 48 (4) ◽  
pp. 1173-1186 ◽  
Author(s):  
Václav Bártl ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Marie Bartošová ◽  
Miroslav Protiva
Keyword(s):  
Acute Toxicity ◽  
Water Soluble ◽  
Hypotensive Activity ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Soluble Salts ◽  
Sleeping Time ◽  
Central Depression ◽  
Derivatives Of ◽  
Electroshock Seizures

Reactions of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins XIVa-XIVd with benzaldehyde, 3,4-dimethoxybenzaldehyde, 4-dimethylaminobenzaldehyde, salicylaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, 2-(2-dimethylaminoethoxy)benzaldehyde, 3-(2-dimethylaminoethoxy)benzaldehyde and 3-ethoxy-4-(2-dimethylaminoethoxy)benzaldehyde afforded a series of 19 hydrazones IIIa-Xc. Some of them showed the expected anticonvulsant effect but only towards pentetrazole; antagonism of maximal electroshock seizures was not observed. In general, the products have a character of tranquillizers: in higher does they produce central depression, potentiate the thiopental sleeping time, have hypothermic action; in single cases antiamphetamine, antireserpine, antihistamine and cataleptic effects were observed. The water-soluble salts of the basic hydrazones VIIIa, VIIIc, IXc and Xc, administered parenterally, showed a rather high acute toxicity and revealed also adrenolytic and hypotensive activity.

scholarly journals Antioxidant Network Based on Sulfonated Polyhydroxyalkanoate and Tannic Acid Derivative

2021 ◽  
Vol 8 (1) ◽  
pp. 9
Author(s):  
Laura Brelle ◽  
Estelle Renard ◽  
Valerie Langlois
Keyword(s):  
Gallic Acid ◽  
Tannic Acid ◽  
Water Soluble ◽  
Gel Formation ◽  
Ene Reaction ◽  
Inorganic Cations ◽  
Medium Chain Length ◽  
Physically Crosslinked ◽  
The Stability ◽  
Derivatives Of

A novel generation of gels based on medium chain length poly(3-hydroxyalkanoate)s, mcl-PHAs, were developed by using ionic interactions. First, water soluble mcl-PHAs containing sulfonate groups were obtained by thiol-ene reaction in the presence of sodium-3-mercapto-1-ethanesulfonate. Anionic PHAs were physically crosslinked by divalent inorganic cations Ca2+, Ba2+, Mg2+ or by ammonium derivatives of gallic acid GA-N(CH3)3+ or tannic acid TA-N(CH3)3+. The ammonium derivatives were designed through the chemical modification of gallic acid GA or tannic acid TA with glycidyl trimethyl ammonium chloride (GTMA). The results clearly demonstrated that the formation of the networks depends on the nature of the cations. A low viscoelastic network having an elastic around 40 Pa is formed in the presence of Ca2+. Although the gel formation is not possible in the presence of GA-N(CH3)3+, the mechanical properties increased in the presence of TA-N(CH3)3+ with an elastic modulus G’ around 4200 Pa. The PHOSO3−/TA-N(CH3)3+ gels having antioxidant activity, due to the presence of tannic acid, remained stable for at least 5 months. Thus, the stability of these novel networks based on PHA encourage their use in the development of active biomaterials.

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