scholarly journals Study of the relationship between geometric isomerism and biologically active properties of compounds

Author(s):  
Arif G. Gasanov ◽  
◽  
Ilgar G. Ayyubov ◽  
Gulsum E. Hajiyeva ◽  
Fidan S. Qurbanova ◽  
...  

The results of the research in the field of studying the relationship of the geometric structure of organic compounds with their biological activity are presented. It has been shown that the stereospecific structure of organic and inorganic molecules can have a direct effect on the biologically active properties of substances. Among the known types of stereoisomerism (geometric and optical), this work summarizes the effect of various types of geometric isomerism on the bioactivity of compounds. In addition, the results of the authors’ own research are presented. In particular, the results of studying the antimicrobial and antifungal activity of hydroxyalkyl monoesters of norbornedicarboxylic acid depending on their stereoisomeric forms in relation to various pathogenic microorganisms are shown. The studies were carried out by the serial dilution method. As nutrient media, we used MPA pH 7,2–7,4 for bacteria and Sabouraud’s medium for fungi. The incubation time in a thermostat for bacteria was 18–24 hours at 37ºC, for fungi 1–10 days at 28ºC. It has been noted that the endo-isomers of the synthesized compounds have a higher antimicrobial and antifungal activity against grampositive (Staphylococcus aureus), gramnegative (Escherichia coli, Pseudomonas aeruginosa) bacteria, as well as yeast-like fungi of the genus Candida. Based on the obtained test reports, the synthesized compounds have been recommended for use as local antiseptic preparations.

2020 ◽  
Vol 17 (34) ◽  
pp. 403-411
Author(s):  
Konul Farrukh BAKHSHALIYEVA ◽  
Nizami Rza NAMAZOV ◽  
Arzu Rasul HASANOVA ◽  
Fidan Rasim MAMMADOVA ◽  
Panah Zulfigar MURADOV

In the carried out of the research, Xylotroph macromycetes have been researched as a perspective producer of bıologıcal actıve substances used for various purposes today in world practice which spread in Azerbaijan and some of their features (the biological activity of synthesized metabolites, toxicity, antimicrobial activity and dynamics of biomass formation ). It became clear that fungi such as Ganoderma lucidum (Curtis) P. Karst., Laetiporus sulphureus (Bull.) Murrill, Pleurotus ostreatus (Jacq.) P. Kumm, Schyzophyllum commune Fr and Trametes versicolor (L.) Lloyd considered as a perspective producer of bıologıcal actıve substances is widely spread in the forests of Azerbaijan, and some of them are even dominant species of xylomicobiot inherent in the nature of Azerbaijan. As a result of studies with isolated strains of these fungi, it was shown that both in the culture solution (CS) and in the vegetative mycelia (VB), there are metabolites with biological activity. The result of research also became clear that antimicrobial activity of CS in all cases is higher than in water or alcohol extracts of dry biomass (1,1-1,2 times), although it defines the overall biological activity of VB extracts to the relationship of Paramecium caudatum gives a higher increase effect. In addition, the selected active strains do not lag behind the known strains in terms of the amount of biomass formed (up to 8.7 g/l in 7 days) and manifestations of forms of biological activity. This gives a serious basis to realize the production of biologically active substances for different (food, feed, medical and other) purposes on their basis.


Author(s):  
HAMZAH JUMAH ESSA BARKAH ◽  
S. LOKESH

Objective: In the present study, emphasis has been made to assay the antifungal activity of some angiospermic epiphytes like Cuscuta reflexa, Viscum orientale, Cymbidium bicolor, Bulbophyllum propinquum, Hoya ovalifolia and Dendrophthoe falcata. Methods: The antifungal activity due to epiphytes extracts was expressed in term of reduction in dry biomass of fungi based on the relationship of ergosterol content and electrolyte leakage in fungal pathogens viz., Colletotrichum dematium, Drechslera oryzae, Fusarium oxysporum and Fusarium solani treated with epiphytes extract. Results: Treated fungi showed increased in ergostesrol content and increased electrolyte leakage confirmed the pathetic situation of fungi; hence there was fungistatic effect, which was dose-dependent. Conclusion: The angiospermic epiphytes of selected species chosen for the study could be serves an alternative eco-friendly source to synthetic fungicides.


2020 ◽  
Vol 99 (3) ◽  
pp. 11-20
Author(s):  
S.D. Fazylov ◽  
◽  
О.А. Nurkenov ◽  
Z.M. Muldakhmetov ◽  
A.M. Gazaliev ◽  
...  

The article presents literature review on the physicochemical and biological properties of fullerene C60, as well as the authors' own experimental data on the synthesis of fullerene derivatives of amines and natural alkaloids. It is shown that the presence of a fullerene fragment in the structure of the compound provides a significant improvement or the appearance of qualitatively new mechanical, chemical, physical, biological and other properties associated with the manifestation of nanoscale factors. The issues of the relationship of the structure, water solubility and biological activity of fullerene С60 derivatives are considered. Many biologically active effects of various modified derivatives of fullerene C60 are described, which have membrane-active, antibacterial, antiviral, immunomodulating, HIV inhibitory enzymes and other properties. It was noted that preparations containing a fullerene fragment are effective against hepatitis C virus, and are also able to efficiently trap free radicals. Derivatives of fullerenes can also be used as antioxidant, neuroprotective and other agents. Particular attention is paid to the authors' own results on the synthesis of amino derivatives of fullerenes.


2018 ◽  
pp. 63-68
Author(s):  
Т. О. Samura

Derivatives of 1,2,4-triazole is a very  perspective class of heterocyclic compounds which have high therapeutic effectiveness. The main direction of research on these derivatives are antifungal, antiviral, antibacterial, soothing, hypnotic, anticonvulsant, anti-inflammatory and other activities. The aim was to analyze literature data and generalize recent advances in the study of antimicrobial and antifungal action of 1,2,4-triazole derivatives which can help to create new biologically active substances of this type of activity. Bibliosemantical method, systems thinking and the results of our own research were used in the work. The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and heteryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized. Some dependence of this type of activity on specialty of chemical structure of heterocyclic system derivatives was specified. Perspective of purposeful synthesis of new derivatives of 1,2,4-triazole and products of their transformation as available object for studying biological activity and expanding knowledge about antimicrobial and antifungal activity of this class of heterocyclic compounds were shown with informational analysis. Topicality and practical importance of finding biologically active compounds and receiving biologically active substance by synthesis of new derivatives of 1,2,4-triazole with high antimicrobial activity in relation to gram-negative and gram-positive bacteria were demonstrated.


2019 ◽  
pp. 96-99
Author(s):  
A. A. Safonov ◽  
Т. V. Panasenko ◽  
E. G. Knysh ◽  
N. M. Polishchuk

For creating a new biologically active compounds are using a system on which already exist medications. One such system is the core of 1,2,4-triazole. The aim of our work was to study the antimicrobial and antifungal activity new 4-((R-iden)amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiols. The study was conducted according to the method of serial dilutions. As a result of studies new synthesized 4-((R-idene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiols exhibit antimicrobial and antifungal activity. The most active compound that exhibits antimicrobial activity against Staphylococcus aureus is 4-((1-(phenyl)ethylidene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiol and 4-((3-nitrobenzylidene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiol, 4-((4-fluorbenzylidene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiol exhibit antifungal activity level of the comparator fluconazole, compound III, VI exceed its performance.


2016 ◽  
Vol 34 (4) ◽  
pp. 675-680 ◽  
Author(s):  
A.Z. SHERAZI ◽  
K. JABEEN ◽  
S. IQBAL ◽  
Z. YOUSAF

ABSTRACT Chenopodium album, leaves were selected to evaluate their antifungal potential against Ascochyta rabiei causative agent for chickpea blight. Different concentrations of methanolic extract of C. album leaves i.e. 1%, 2.5%, 4%, 5.5% and 7% were tested against the target fungus A. rabiei. Maximum reduction in the test fungal biomass (68%) was observed in 7% concentration. This methanolic leaf extract was partitioned and n-butanol, chloroform, n-hexane, ethyl acetate fractions were isolated according to their polarity. In vitro antifungal activity of these fractions was studied by serial dilution method. n-hexane fraction exhibited the highest antifungal potential with 55% inhibition in test fungal biomass, so this fraction was selected for Gas chromatography mass spectrometry (GC-MS) analysis. Total thirteen compounds identified in this analysis belonged to class aromatic hydrocarbons, hydrocarbons, saturated fatty acids, aromatic carboxylic acid, siloxanes, phosphonates and cardiac glycosides. These compounds might be responsible for antifungal activity of C. album.


Paleobiology ◽  
1980 ◽  
Vol 6 (02) ◽  
pp. 146-160 ◽  
Author(s):  
William A. Oliver

The Mesozoic-Cenozoic coral Order Scleractinia has been suggested to have originated or evolved (1) by direct descent from the Paleozoic Order Rugosa or (2) by the development of a skeleton in members of one of the anemone groups that probably have existed throughout Phanerozoic time. In spite of much work on the subject, advocates of the direct descent hypothesis have failed to find convincing evidence of this relationship. Critical points are:(1) Rugosan septal insertion is serial; Scleractinian insertion is cyclic; no intermediate stages have been demonstrated. Apparent intermediates are Scleractinia having bilateral cyclic insertion or teratological Rugosa.(2) There is convincing evidence that the skeletons of many Rugosa were calcitic and none are known to be or to have been aragonitic. In contrast, the skeletons of all living Scleractinia are aragonitic and there is evidence that fossil Scleractinia were aragonitic also. The mineralogic difference is almost certainly due to intrinsic biologic factors.(3) No early Triassic corals of either group are known. This fact is not compelling (by itself) but is important in connection with points 1 and 2, because, given direct descent, both changes took place during this only stage in the history of the two groups in which there are no known corals.


Author(s):  
D. F. Blake ◽  
L. F. Allard ◽  
D. R. Peacor

Echinodermata is a phylum of marine invertebrates which has been extant since Cambrian time (c.a. 500 m.y. before the present). Modern examples of echinoderms include sea urchins, sea stars, and sea lilies (crinoids). The endoskeletons of echinoderms are composed of plates or ossicles (Fig. 1) which are with few exceptions, porous, single crystals of high-magnesian calcite. Despite their single crystal nature, fracture surfaces do not exhibit the near-perfect {10.4} cleavage characteristic of inorganic calcite. This paradoxical mix of biogenic and inorganic features has prompted much recent work on echinoderm skeletal crystallography. Furthermore, fossil echinoderm hard parts comprise a volumetrically significant portion of some marine limestones sequences. The ultrastructural and microchemical characterization of modern skeletal material should lend insight into: 1). The nature of the biogenic processes involved, for example, the relationship of Mg heterogeneity to morphological and structural features in modern echinoderm material, and 2). The nature of the diagenetic changes undergone by their ancient, fossilized counterparts. In this study, high resolution TEM (HRTEM), high voltage TEM (HVTEM), and STEM microanalysis are used to characterize tha ultrastructural and microchemical composition of skeletal elements of the modern crinoid Neocrinus blakei.


Author(s):  
Leon Dmochowski

Electron microscopy has proved to be an invaluable discipline in studies on the relationship of viruses to the origin of leukemia, sarcoma, and other types of tumors in animals and man. The successful cell-free transmission of leukemia and sarcoma in mice, rats, hamsters, and cats, interpreted as due to a virus or viruses, was proved to be due to a virus on the basis of electron microscope studies. These studies demonstrated that all the types of neoplasia in animals of the species examined are produced by a virus of certain characteristic morphological properties similar, if not identical, in the mode of development in all types of neoplasia in animals, as shown in Fig. 1.


Author(s):  
J.R. Pfeiffer ◽  
J.C. Seagrave ◽  
C. Wofsy ◽  
J.M. Oliver

In RBL-2H3 rat leukemic mast cells, crosslinking IgE-receptor complexes with anti-IgE antibody leads to degranulation. Receptor crosslinking also stimulates the redistribution of receptors on the cell surface, a process that can be observed by labeling the anti-IgE with 15 nm protein A-gold particles as described in Stump et al. (1989), followed by back-scattered electron imaging (BEI) in the scanning electron microscope. We report that anti-IgE binding stimulates the redistribution of IgE-receptor complexes at 37“C from a dispersed topography (singlets and doublets; S/D) to distributions dominated sequentially by short chains, small clusters and large aggregates of crosslinked receptors. These patterns can be observed (Figure 1), quantified (Figure 2) and analyzed statistically. Cells incubated with 1 μg/ml anti-IgE, a concentration that stimulates maximum net secretion, redistribute receptors as far as chains and small clusters during a 15 min incubation period. At 3 and 10 μg/ml anti-IgE, net secretion is reduced and the majority of receptors redistribute rapidly into clusters and large aggregates.


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