scholarly journals Synthesis and therapeutic potential of imidazole containing compounds

BMC Chemistry ◽  
2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Ankit Siwach ◽  
Prabhakar Kumar Verma
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Biological Properties ◽  
New Drugs ◽  
Hydrogen Atoms ◽  
Tautomeric Forms ◽  
Synthetic Routes ◽  
Derivatives Of ◽  
Heterocyclic Moiety ◽  
Antihistaminic Agent

Abstract Imidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen. The imidazole name was reported by Arthur Rudolf Hantzsch (1857–1935) in 1887. 1, 3-diazole is an amphoteric in nature i.e. it shows both acidic and basic properties. It is a white or colorless solid that is highly soluble in water and other polar solvents. Due to the presence of a positive charge on either of two nitrogen atom, it shows two equivalent tautomeric forms. Imidazole was first named glyoxaline because the first synthesis has been made by glyoxal and ammonia. It is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. The derivatives of 1, 3-diazole show different biological activities such as antibacterial, antimycobacterial, anti-inflammatory, antitumor, antidiabetic, anti-allergic, antipyretic, antiviral, antioxidant, anti-amoebic, antihelmintic, antifungal and ulcerogenic activities, etc. as reported in the literature. There are different examples of commercially available drugs in the market which contains 1, 3-diazole ring such as clemizole (antihistaminic agent), etonitazene (analgesic), enviroxime (antiviral), astemizole (antihistaminic agent), omeprazole, pantoprazole (antiulcer), thiabendazole (antihelmintic), nocodazole (antinematodal), metronidazole, nitroso-imidazole (bactericidal), megazol (trypanocidal), azathioprine (anti rheumatoid arthritis), dacarbazine (Hodgkin's disease), tinidazole, ornidazole (antiprotozoal and antibacterial), etc. This present review summarized some pharmacological activities and various kinds of synthetic routes for imidazole and their derived products.

scholarly journals Therapeutic potential of oxadiazole or furadiazole containing compounds

BMC Chemistry ◽  
2020 ◽  
Vol 14 (1) ◽  
Author(s):  
Ankit Siwach ◽  
Prabhakar Kumar Verma
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Antiviral Drug ◽  
Biological Properties ◽  
New Drugs ◽  
Pharmacological Activities ◽  
Methylene Groups ◽  
Synthetic Routes ◽  
Azole Ring ◽  
Derivatives Of

AbstractAs we know that, Oxadiazole or furadi azole ring containing derivatives are an important class of heterocyclic compounds. A heterocyclic five-membered ring that possesses two carbons, one oxygen atom, two nitrogen atoms, and two double bonds is known as oxadiazole. They are derived from furan by the replacement of two methylene groups (= CH) with two nitrogen (-N =) atoms. The aromaticity was reduced with the replacement of these groups in the furan ring to such an extent that it shows conjugated diene character. Four different known isomers of oxadiazole were existed such as 1,2,4-oxadiazole, 1,2,3-oxadiazole, 1,2,5-oxadiazole & 1,3,4-oxadiazole. Among them, 1,3,4-oxadiazoles & 1,2,4-oxadiazoles are better known and more widely studied by the researchers due to their broad range of chemical and biological properties. 1,3,4-oxadiazoles have become important synthons in the development of new drugs. The derivatives of the oxadiazole nucleus (1,3,4-oxadiazoles) show various biological activities such as antibacterial, anti-mycobacterial, antitumor, anti-viral and antioxidant activity, etc. as reported in the literature. There are different examples of commercially available drugs which consist of 1,3,4-oxadiazole ring such as nitrofuran derivative (Furamizole) which has strong antibacterial activity, Raltegravir as an antiviral drug and Nesapidil drug is used in anti-arrhythmic therapy. This present review summarized some pharmacological activities and various kinds of synthetic routes for 2, 5-disubstituted 1,3,4-oxadiazole, and their derived products.

scholarly journals Monoterpenes and Sesquiterpenes of Essential Oils from Psidium Species and Their Biological Properties

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 965
Author(s):  
Renan Campos e Silva ◽  
Jamile S. da Costa ◽  
Raphael O. de Figueiredo ◽  
William N. Setzer ◽  
Joyce Kelly R. da Silva ◽  
...  
Keyword(s):  
Essential Oils ◽  
Biological Activities ◽  
Biological Properties ◽  
Chemical Diversity ◽  
New Drugs ◽  
Natural Sources ◽  
Biological Potential ◽  
The World ◽  
Review Reports ◽  
Collection Sites

Psidium (Myrtaceae) comprises approximately 266 species, distributed in tropical and subtropical regions of the world. Psidium taxa have great ecological, economic, and medicinal relevance due to their essential oils’ chemical diversity and biological potential. This review reports 18 Psidium species growing around the world and the chemical and biological properties of their essential oils. Chemically, 110 oil records are reported with significant variability of volatile constituents, according to their seasonality and collection sites. Monoterpenes and sesquiterpenes with acyclic (C10 and C15), p-menthane, pinane, bisabolane, germacrane, caryophyllane, cadinane, and aromadendrane skeleton-types, were the primary constituents. The essential oils showed various biological activities, including antioxidant, antifungal, antibacterial, phytotoxic, larvicidal, anti-inflammatory, and cytotoxic properties. This review contributes to the Psidium species rational and economic exploration as natural sources to produce new drugs.

Phytochemical content and potential health applications of pecan [Carya illinoinensis (Wangenh) K. Koch] nutshell

2022 ◽  
Vol 22 ◽  
Author(s):  
Nohemí del C. Reyes-Vázquez ◽  
Laura A. de la Rosa ◽  
Juan Luis Morales-Landa ◽  
Jorge Alberto García-Fajardo ◽  
Miguel Ángel García-Cruz
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Heart Diseases ◽  
Extraction Methods ◽  
New Drugs ◽  
Potential Health ◽  
In Vivo Models ◽  
Phytochemical Content ◽  
Pecan Nutshell

Background: The pecan nutshell contains phytochemicals with various biological activities that are potentially useful in the prevention or treatment of diseases such as cancer, diabetes, and metabolic imbalances associated with heart diseases. Objective: To update this topic by means of a literature review and include those that contribute to the knowledge of the chemical composition and biological activities of pecan nutshell, particularly of those related to the therapeutic potential against some chronic degenerative diseases associated with oxidative stress. Method: Exhaustive and detailed review of the existing literature using electronic databases. Conclusion: The pecan nutshell is a promising natural product with pharmaceutical uses in various diseases. However, additional research related to the assessment of efficient extraction methods and characterization, particularly the evaluation of the mechanisms of action in new in vivo models, is necessary to confirm these findings and development of new drugs with therapeutic use.

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

scholarly journals Isatis tinctoria L. (Woad): A Review of Its Botany, Ethnobotanical Uses, Phytochemistry, Biological Activities, and Biotechnological Studies

Plants ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 298 ◽  
Author(s):  
Jasmine Speranza ◽  
Natalizia Miceli ◽  
Maria Fernanda Taviano ◽  
Salvatore Ragusa ◽  
Inga Kwiecień ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Raw Material ◽  
Future Research ◽  
Shoot Cultures ◽  
Isatis Tinctoria ◽  
Enhanced Production

Isatis tinctoria L. (Brassicaceae), which is commonly known as woad, is a species with an ancient and well-documented history as an indigo dye and medicinal plant. Currently, I. tinctoria is utilized more often as medicinal remedy and also as a cosmetic ingredient. In 2011, I. tinctoria root was accepted in the official European phytotherapy by introducing its monograph in the European Pharmacopoeia. The biological properties of raw material have been known from Traditional Chinese Medicine (TCM). Over recent decades, I. tinctoria has been investigated both from a phytochemical and a biological point of view. The modern in vitro and in vivo scientific studies proved anti-inflammatory, anti-tumour, antimicrobial, antiviral, analgesic, and antioxidant activities. The phytochemical composition of I. tinctoria has been thoroughly investigated and the plant was proven to contain many valuable biologically active compounds, including several alkaloids, among which tryptanthrin, indirubin, indolinone, phenolic compounds, and polysaccharides as well as glucosinolates, carotenoids, volatile constituents, and fatty acids. This article provides a general botanical and ethnobotanical overview that summarizes the up-to-date knowledge on the phytochemistry and biological properties of this valuable plant in order to support its therapeutic potential. Moreover, the biotechnological studies on I. tinctoria, which mainly focused on hairy root cultures for the enhanced production of flavonoids and alkaloids as well as on the establishment of shoot cultures and micropropagation protocols, were reviewed. They provide input for future research prospects.

scholarly journals Propolis: A Complex Natural Product with a Plethora of Biological Activities That Can Be Explored for Drug Development

2015 ◽  
Vol 2015 ◽  
pp. 1-29 ◽  
Author(s):  
Ricardo Silva-Carvalho ◽  
Fátima Baltazar ◽  
Cristina Almeida-Aguiar
Keyword(s):  
Chemical Composition ◽  
Biological Activities ◽  
Clinical Effectiveness ◽  
Biological Properties ◽  
New Drugs ◽  
Published Data ◽  
Alternative Source ◽  
Scientific Attention

The health industry has always used natural products as a rich, promising, and alternative source of drugs that are used in the health system. Propolis, a natural resinous product known for centuries, is a complex product obtained by honey bees from substances collected from parts of different plants, buds, and exudates in different geographic areas. Propolis has been attracting scientific attention since it has many biological and pharmacological properties, which are related to its chemical composition. Severalin vitroandin vivostudies have been performed to characterize and understand the diverse bioactivities of propolis and its isolated compounds, as well as to evaluate and validate its potential. Yet, there is a lack of information concerning clinical effectiveness. The goal of this review is to discuss the potential of propolis for the development of new drugs by presenting published data concerning the chemical composition and the biological properties of this natural compound from different geographic origins.

scholarly journals Dendropanax Morbiferus and Other Species from the Genus Dendropanax: Therapeutic Potential of Its Traditional Uses, Phytochemistry, and Pharmacology

Antioxidants ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 962
Author(s):  
Rengasamy Balakrishnan ◽  
Duk-Yeon Cho ◽  
In Su-Kim ◽  
Dong-Kug Choi
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Safety Evaluation ◽  
Biological Properties ◽  
Comprehensive Analysis ◽  
Flowering Plant ◽  
High Concentration ◽  
Medicinal Uses ◽  
Wide Range ◽  
Bioactive Ingredients

The Dendropanax genus is a kind of flowering plant in the family of Araliaceae that encompasses approximately 91 to 95 species. Several Dendropanax species are used as traditional medicinal plants, extensively used Korea and South America and other parts of the world. Almost every part of the plant, including the leaves, bark, roots, and stems, can be used as traditional medicine for the prevention and management of a broad spectrum of health disorders. This paper sought to summarizes the ethnopharmacological benefits, biological activities, and phytochemical investigations of plants from the genus Dendropanax, and perhaps to subsequently elucidate potential new perspectives for future pharmacological research to consider. Modern scientific literature suggests that plants of the Dendropanax genus, together with active compounds isolated from it, possess a wide range of therapeutic and pharmacological applications, including antifungal, anti-complement, antioxidant, antibacterial, insect antifeedant, cytotoxic, anti-inflammatory, neuroprotective, anti-diabetic, anti-cancer, and anti-hypouricemic properties. The botanical descriptions of approximately six to 10 species are provided by different scientific web sources. However, only six species, namely, D. morbiferus, D. gonatopodus, D. dentiger, D. capillaris, D. chevalieri, and D. arboreus, were included in the present investigation to undergo phytochemical evaluation, due to the unavailability of data for the remaining species. Among these plant species, a high concentration of variable bioactive ingredients was identified. In particular, D. morbifera is a traditional medicinal plant used for the multiple treatment purposes and management of several human diseases or health conditions. Previous experimental evidence supports that the D. morbifera species could be used to treat various inflammatory disorders, diarrhea, diabetes, cancer, and some microbial infections. It has recently been reported, by our group and other researchers, that D. morbifera possesses a neuroprotective and memory-enhancing agent. A total of 259 compounds have been identified among six species, with 78 sourced from five of these species reported to be bioactive. However, there is no up-to-date information concerning the D. morbifera, its different biological properties, or its prospective benefits in the enhancement of human health. In the present study, we set out to conduct a comprehensive analysis of the botany, traditional medicinal history, and medicinal resources of species of the Dendropanax genus. In addition, we explore several phytochemical constituents identified in different species of the Dendropanax genus and their biological properties. Finally, we offer comprehensive analysis findings of the phytochemistry, medicinal uses, pharmacological actions, and a toxicity and safety evaluation of the D. morbifera species and its main bioactive ingredients for future consideration.

scholarly journals The growth-inhibitory and carcinogenic properties of 4-aminostilbene and derivatives

1948 ◽  
Vol 241 (830) ◽  
pp. 147-195 ◽  
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Essential Feature ◽  
Phenyl Group ◽  
Great Majority ◽  
Biological Properties ◽  
Hydrogen Atoms ◽  
Ethylene Bridge ◽  
Growth Inhibitory ◽  
Carcinogenic Action

Marked inhibition of the growth of the Walker rat carcinoma 256 is produced by administration of 4-aminostilbene and of 4-dimethylaminostilbene. From similar experiments with the Crocker sarcoma 180, the carcinoma C63, and spontaneous mammary cancer, it appears that the growth inhibitory action of these compounds is much less pronounced in mice. In a dosage of 200 to 250 mg. /kg. in the rat, both 4-amino- and 4-dimethylaminostilbene produce ( a ) gastro-intestinal submucous haemorrhage most evident in the pyloric portion of the stomach, ( b ) haematuria, and ( c ) haemolymph changes, while the former compound induces methaemoglobinaemia in addition. Using the Walker rat carcinoma 256 as the biological test object, a series of derivatives of 4-aminostilbene has been examined to determine the relationship between the growth-inhibitory effect and chemical constitution. The great majority of the active compounds can be defined as stilbenes with a basic substituent, the position of which is of paramount importance; thus o -dimethylaminostilbene is very much less active than the p -isomeride, and the m -compound is completely inactive. A further essential feature is the ethylene bridge, since activity disappears when either of its hydrogen atoms is substituted, when the bridge is reduced, when it is extended to contain three or four carbon atoms, or when either methine group is replaced by a nitrogen atom. Compounds in which the ethylene bridge is absent, or is replaced by oxygen or sulphur, are also inactive, and activity is further dependent upon the trans configuration of the molecule about the ethylenic bond, and to a large extent upon a free p' -position. These and other facts have suggested the working hypothesis that one of the features required for activity is an unbroken conjugation of the amino group with both nuclei, enabling the compound to assume some dipolar quinonoid character, which depends, among other things, on the co-planar arrangement of the two benzene nuclei which characterizes the trans form of the stilbenes. When evidence concerning steric conditions in the molecules (obtained mainly from the ultraviolet spectroscopy of 4-dimethylaminostilbene and thirteen of its alkyl derivatives) is compared with the biological activities of these compounds, a close parallel is suggested between lack of growth-inhibitory power and buckling of the molecule. Thus in the 4-dimethylaminostilbene derivatives with substituents on the x- and ?-carbon atoms of the ethylenic double bond, or with methyl groups at two ortho positions in a phenyl group, steric factors reduce the planarity of the molecule, thus affecting the conjugation resonance characteristic of the whole molecule. These compounds had previously been found to be non-inhibitory. All the evidence from diagrams, models and spectra suggests that steric interference with the planar configuration of molecules in this series varies continuously from the planar 4-dimethylaminostilbene to the highly buckled a/?-diethyl derivative. Inhibitory activity within this series appears to depend upon a conjunction of such factors as molecular size and shape, and the apposition of a planar molecule to a hypothetical adsorbing surface. In view of the previously suggested connexion between growth-inhibitory activity and tumour production, a number of selected aminostilbenes has been tested for carcinogenicity. Of seventy-two rats exposed to the action of 4-amino-, 4-acetamido-, 4-dimethylamino-, or 4-diethyIaminostilbene, twenty-three developed a total of eight sarcomata and thirty distant tumours mostly comprising squamous keratinizing carcinomata of the external acoustic duct, mammary adenomata, and cholangiomata. In a second series, the compounds 4-amino-, 4-dimethylamino- and 2,-methyl- 4-dimethylaminostilbene, and 1-(4'-dimethylaminophenyl)-2-(T-naphthyl)ethylene, were tested in male and female mice and rats. Of 120 rats exposed, forty-eight developed a total of twenty sarcomata at the site of injection and fifty-one tumours in organs distant from the site of injection, while of 120 mice similarly treated only four sarcomata and two distant tumours were recorded in five. The nature and distribution of the distant tumours induced in the rat strongly suggest some common feature in the carcinogenic action of aminostilbenes and 2-acetamidofluorene. Other points discussed include ( a ) the association between haemolymphatic changes and carcinogenesis, ( b ) the possible significance of the nitrogenous analogue 2-(4'-dimethylaminostyryl) quinoline in relation to the carcinogenic action of ‘styryl 430’, ( c ) a comparison of the biological properties of 4-dimethylaminostilbene and 4-dimethylaminoazobenzene, and ( d ) the dependence for manifestation of the growth-inhibiting action of the aminostilbenes upon a sufficiently low intake of dietary protein.

scholarly journals IN SILICO STUDIES OF SOPHORAFLAVANONE G: QUANTUM CHARACTERIZATION AND ADMET

2020 ◽  
Vol 7 (11) ◽  
pp. 160-179 ◽  
Author(s):  
David Lopes Santiago De Oliveira ◽  
Emanuelle Machado Marinho ◽  
Francisco Nithael Melo Lucio ◽  
Marcia Machado Marinho ◽  
Francisco Rogênio Da Silva Mendes ◽  
...  
Keyword(s):  
Estrogen Receptor Alpha ◽  
Therapeutic Potential ◽  
Early Stage ◽  
Biological Activities ◽  
Three Dimensional ◽  
New Drugs ◽  
Dimensional Structure ◽  
Skin Permeability ◽  
Biological Targets ◽  
In Silico Studies

Currently, the search for new drugs with greater therapeutic potential and less side effects has been fostered by the advancement of the use of molecular modeling drugs, which in addition to supporting the full characterization of the molecule, allow simple algorithms to predict pharmacokinetic. In this context the present work aimed to perform the electronic / structural characterization, to evaluate the pharmacokinetic properties and to perform a virtual screening of the possible biological targets of Sophoraflavonone G, a promising flavonone, which presents several pharmacological properties. Sophoraflavanone G was geometrically optimized by semi-empirical quantum calculations, plot the MESP, identifying the nucleophilic sites. Using the boundary orbitals, it was possible to identify a greater tendency for electron donation in relation to Naringeni, with lower ionization potential, higher hardness and less softness. With respect to pharmacokinetics Sophoraflavonone G confirmed the safety of the compound for oral administration with good skin permeability, which allows applications in topical formulations. Presents indications for gastro intestinal absorption, as for possible interactions with biological targets, interaction with the estrogen receptor alpha, sodium / glucose co-transporter 2, beta-secretase 1, cyclooxygenase-1.The data obtained from an early stage for a comparative analysis between its analogues and fundamental for future studies of relationships between the three-dimensional structure of Sophoraflavanone G and its biological activities.

Advances on Monosaccharides and Oligosaccharides: Structural Modifications and Bioactivities

2021 ◽  
Vol 21 ◽  
Author(s):  
Shaochen Li ◽  
Min Lv ◽  
Shaoyong Zhang ◽  
Hui Xu
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Biological Activities ◽  
Building Blocks ◽  
Biological Properties ◽  
Mechanisms Of Action ◽  
Biological Processes ◽  
Structural Modifications ◽  
Structure Activity ◽  
Derivatives Of

: Derivatives of monosaccharides and oligosaccharides play the important roles in biological processes. Monosaccharides are the single carbohydrate building blocks, such as glucose, xylose, and fructose. Oligosaccharides are composed of 2–10 monosaccharides including disaccharides and trisaccharides. Moreover, monosaccharides, oligosaccharides and their derivatives are vital molecules with various biological properties including anticancer activity, antiviral activity, insecticidal activity, antimicrobial activity, and antioxidant activity. This review covers a survey of structural modifications, biological activities, and mechanisms of action of monosaccharides, oligosaccharides and their derivatives. Additionally, their structure–activity relationships are also concluded.

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