1,2,3-Triazole- and Quinoline-Based Hybrids with Potent Antiplasmodial Activity

2021 ◽  
Vol 18 ◽  
Author(s):  
Isabela A. Graciano ◽  
Alcione S. de Carvalho ◽  
Fernando de Carvalho da Silva ◽  
Vitor F. Ferreira
Keyword(s):  
Antimalarial Activity ◽  
Biological Activities ◽  
Review Article ◽  
Pharmaceutical Market ◽  
Biologically Active ◽  
New Drugs ◽  
Synthetic Methods ◽  
Antiplasmodial Activity ◽  
New Chemical Entities ◽  
Active Substances

Background: Malaria is a disease causing millions of victims every year and requires new drugs, often due to parasitic strain mutations. Thus, the search for new molecules that possess antimalarial activity is constant and extremely important. However, the potential that an antimalarial drug possesses cannot be ignored, and molecular hybridization is a good strategy to design new chemical entities. Objective: This review article aims to emphasize recent advances in the biological activities of new 1,2,3-triazole- and quinoline-based hybrids and their place in the development of new biologically active substances. More specifically, it intends to present the synthetic methods that have been utilized for the syntheses of hybrid 1,2,3-triazoles with quinoline nuclei. Method: We have comprehensively and critically discussed all the information available in the literature regarding 1,2,3-triazole- and quinoline-based hybrids with potent antiplasmodial activity. Results: The quinoline nucleus has already been proven to lead to new chemical entities in the pharmaceutical market, such as drugs for the treatment of malaria and other diseases. The same can be said about the 1,2,3-triazole heterocycle, which has been shown to be a beneficial scaffold for the construction of new drugs with several activities. However, only a few triazoles have entered the pharmaceutical market as drugs. Conclusion: Many studies have been conducted to develop new substances that may circumvent the resistance developed by the parasite that causes malaria, thereby improving the therapy currently used.

An Update on the Synthesis and Applications of Bis(Naphthoquinones): An Important Class of Molecules against Infectious Diseases and Other Conditions

2021 ◽  
Vol 21 ◽  
Author(s):  
Luana da S. M. Forezi ◽  
Acácio S. de Souza ◽  
Carolina G. S. Lima ◽  
Amanda A. Borges ◽  
Patricia G. Ferreira ◽  
...  
Keyword(s):  
Infectious Diseases ◽  
General Class ◽  
Biological Activities ◽  
Pharmaceutical Market ◽  
Synthetic Methods ◽  
Important Class ◽  
Biological Targets ◽  
Valuable Compounds ◽  
Synthetic Approaches

: Naphthoquinones are important molecules belonging to the general class of quinones, and many of these compounds have become drugs that are in the pharmaceutical market for the treatment of several diseases. A special subclass of compounds is that of the bis(naphthoquinones), which have two linked naphthoquinone units. In the last few years, several synthetic approaches toward such valuable compounds have been described, as well as their evaluation against numerous important biological targets. In this review, we provide a thorough discussion on the various synthetic methods reported for the synthesis of bis(naphthoquinone) analogues, also highlighting the biological activities of these substances.

scholarly journals In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues

2020 ◽  
Author(s):  
Fidelia Ijeoma Uche ◽  
Xiaozhen Guo ◽  
Jude Okokon ◽  
Imran Ullah ◽  
Paul Horrocks ◽  
...  
Keyword(s):  
Metabolic Pathways ◽  
High Performance ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Antiplasmodial Activity ◽  
Survival Times ◽  
Antiproliferative Effects ◽  
Future Evaluation

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2′-norcocsuline (3)) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semi-synthetic analogues (4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR Green 1 fluorescence assay. The in vivo antimalarial activity of cycleanine (1) is then investigated in suppressive, prophylactic and curative murine malaria models after infection with a chloroquine-sensitive Plasmodium berghei strain. BBIQ alkaloids (1–5) exerted in vitro antiplasmodial activities with IC50 at low micromolar concentrations with the two semi-synthetic cycleanine analogues showing an improved potency and selectivity than cycleanine. At oral doses of 25 and 50mg/kg body weight of infected mice, cycleanine suppressed the levels of parasitaemia, and increased mean survival times significantly compared to the control groups. The metabolites and metabolic pathways of cycleanine (1) were also studied using high performance liquid chromatography electrospray ionization tandem mass spectrometry. Twelve novel metabolites were detected in rats after intragastic administration of cycleanine. The metabolic pathways of cycleanine were demonstrated to involve hydroxylation, dehydrogenation, and demethylation. Overall, these in vitro and in vivo results provide a basis for the future evaluation of cycleanine and its analogues as leads for further development.

scholarly journals Justification of the effectiveness of hirudotherapy in dentistry

2020 ◽  
Vol 24 (5) ◽  
pp. 328-331
Author(s):  
A. I. Abdullaeva ◽  
Elena P. Pustovaya ◽  
V. M. Slonova ◽  
A. S. Karnaeva ◽  
O. V. Pilshchikova ◽  
...  
Keyword(s):  
Web Of Science ◽  
Factor Xa ◽  
Biologically Active ◽  
New Drugs ◽  
Factor Xa Inhibitor ◽  
Complex Treatment ◽  
Periodontal Tissues ◽  
Salivary Gland Secretion ◽  
Methods Of Treatment ◽  
Active Substances

This article provides a systematic review of studies on the composition of leech saliva secretions, the method of hirudotherapy, and the results of hirudotherapy in complex treatment. The following databases were used to search for the study: Scopus, Web of Science, MedLine, and Global Health. When using known methods of treatment, there is often no stability of results, this is explained by the search for new drugs and methods for treating periodontitis. It is known that the secret of the salivary glands of the medical leech contains more than 100 biologically active substances. The therapeutic effect of hirudotherapy is associated with the mechanical discharge of blood flow and the action of a complex salivary gland secretion of a medical leech. The molecules that exist in leech saliva and are the most studied to date include active substances such as hyaluronidase, hirudin, Kalin, destabilase, bdellins, histamine-like substances, hirustazine, factor XA inhibitor, and collagenase. It is scientifically proven that hirudotherapy leads to a significant improvement in the clinical condition of periodontal tissues, is simple, accessible, and can be recommended for use in the practice of periodontists.

Green Chemistry Approaches to the Synthesis of Coumarin Derivatives

2020 ◽  
Vol 24 (1) ◽  
pp. 4-43 ◽  
Author(s):  
Maja Molnar ◽  
Melita Lončarić ◽  
Marija Kovač
Keyword(s):  
Energy Consumption ◽  
Green Chemistry ◽  
Biological Activities ◽  
Daily Basis ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Specific Class ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Coumarin Synthesis

This review is a compilation of the green synthetic methods used in the synthesis of coumarin derivatives. Coumarins are a class of compounds with a pronounced wide range of biological activities, which have found their application in medicine, pharmacology, cosmetics and food industry. Their biological activity and potential application are highly dependent on their structure. Therefore, many researchers have been performing the synthesis of coumarin derivatives on a daily basis. High demands for their synthesis often result in an increased generation of different waste chemicals. In order to minimize the utilization and generation of toxic organic substances, green synthetic methods are applied in this manner. These methods are getting more attention in the last few decades. Green chemistry methods cover a wide range of methods, including the application of ultrasound and microwaves, ionic liquids and deep eutectic solvents, solvent-free synthesis, mechanosynthesis and multicomponent reactions. All typical condensation reactions for coumarin synthesis like Knoevenagel, Perkin, Kostanecki-Robinson, Pechmann and Reformansky reactions, have been successfully performed using these green synthetic methods. According to the authors mentioned in this review, not only these methods reduce the utilization and generation of toxic chemicals, but they can also enhance the reaction performance in terms of product yields, purity, energy consumption and post-synthetic procedures when compared to the conventional methods. Due to the significance of coumarins as biologically active systems and the recent demands of reducing toxic solvents, catalysts and energy consumption, this review provides a first full literature overview on the application of green synthetic methods in the coumarin synthesis. It covers a literature search over the period from 1995-2019. The importance of this work is its comprehensive literature survey on a specific class of heterocyclic compounds, and those researchers working on the coumarin synthesis can find very useful information on the green synthetic approaches to their synthesis. There are some reviews on the coumarin synthesis, but most of them cover only specific reactions on coumarin synthesis and none of them the whole range of green chemistry methods.

The Fungal Metabolites with Potential Antiplasmodial Activity

2018 ◽  
Vol 25 (31) ◽  
pp. 3796-3825 ◽  
Author(s):  
Bin Yang ◽  
Jingxia Huang ◽  
Xuefeng Zhou ◽  
Xiuping Lin ◽  
Juan Liu ◽  
...  
Keyword(s):  
Natural Products ◽  
Antimicrobial Agents ◽  
Antimalarial Activity ◽  
Management Strategies ◽  
Marine Fungus ◽  
Chemical Diversity ◽  
Biologically Active ◽  
Antiplasmodial Activity ◽  
Marine Environments ◽  
Tropical Regions

Malaria caused by Plasmodium parasites is amongst many prevalent public health concerns in several tropical regions of the world. Nowadays, the parasite resistance patterns to most currently used drugs in therapy and insecticides have created an urgent need for new chemical entities exhibiting new modes of action and management strategies. Fungus has been proven to be an excellent source of biologically active compounds, which have been screened for antiplasmodial activity as potential sources of new antimalarial drugs. This review summarizes the current 255 natural products from fungus, which may possess antimalarial activity and can be classified as sesquiterpenes, diterpenes, sesterterpenes, alkaloids, peptides depsipeptides, xanthones, anthraquinones, anthrones, bioxanthracenes, bixanthones, preussomerins, depsidones, phenols, trichothecenes, azaphliones, macrolides, and steroids. However, the treatments available for malaria are limited. Thus, the identification of novel antimicrobial agents should be continued, and all possible strategies should be explored. Carrying forward the antimalarial screening in exited terrestrial and marine natural products library, and finding the new natural products in new resources, particularly those living in marine environments, are still important approaches to find new antimalarial agents. Unusual marine environments are associated with chemical diversity, leading to a resource of novel active substances for the development of bioactive products. Finding new antimalarial natural products in marine fungus, particularly those living in deep-sea and special marine environments, is an important approach to identify novel active agents.

scholarly journals MUSCARI ARMENIACUM LEICHTLIN (GRAPE HYACINTH): PHYTOCHEMISTRY AND BIOLOGICAL ACTIVITIES REVIEW

2019 ◽  
Vol 12 (1) ◽  
pp. 68
Author(s):  
Dmitry Olegovich Bokov
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Antimutagenic Activity ◽  
Therapeutic Effects ◽  
Herbal Drug ◽  
Ribosome Inactivating Proteins ◽  
Phytochemical Studies ◽  
Active Substances

This review focuses on the Muscari armeniacum Leichtlin (Asparagaceae Juss) biologically active substances composition presented in the Aireal and underground parts and finding their possible therapeutic effects. The systematic review is dedicated to the composition of biologically active substances, including recent advances in the biological activity investigation, phytochemical studies, and biotechnology methods of plant material producing. Various electronic search engines such as Google, Google Scholar, scientific literature, publishing sites, and electronic databases such as PubMed, Wiley, Springer, and Science Direct had been searched and data obtained. Other online academic libraries such as E-library and specific ethnopharmacological literature had been searched systematically for more exhaustive information on the crude herbal drug. The chemical composition of M. armeniacum biologically active substances is established; it contains anthocyanins (delphinidin and cyanidin derivatives), homoisoflavonoids, polyhydroxylated pyrrolizidine alkaloids (hyacinthacines A1, A2, A3, and B3), oligoglycosides (Muscarosides), and ribosome-inactivating proteins (musarmins). Recent physicochemical analytical procedures for components determination and hyacinthacines synthesis pathways are mentioned. Moreover, future prospects and trends in the research of this plant have been proposed. We have reviewed researches conducted on M. armeniacum especially in areas of its use in medicine, phytochemicals, biological activity, and developed analytical methods. M. armeniacum possesses antioxidant, antimutagenic activity, and specific glycosidase inhibitory activity; M. armeniacum can be used for the production of potential anticancer, antiviral, antidiabetic, and anti-obesity drugs. It should be noted that more pharmacognostic, pharmacological studies are needed for giving further information on the clinical practice and standardization procedures for the crude herbal drug.

scholarly journals Элеутерококк колючий – популярный адаптоген Дальнего Востока. Сообщение 2 «Ресурсы, опыт интродукции и культивирования. Стандартизация сырья»

2019 ◽  
pp. 107-112
Keyword(s):  
Raw Materials ◽  
Far East ◽  
Growth Conditions ◽  
Review Article ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Eleutherococcus Senticosus ◽  
The Far East ◽  
Active Substances

The review article presents the results of the analysis of literature data on the study of the Eleutherococcus senticosus resources in the Far East. It includes information on the results of its introduction and cultivation as well as the study of the content of biologically active substances in relation to different growth conditions. The article describes the differences in pharmacopoeial methods for assessing the quality of raw materials for Eleutherococcus senticosus in Russia and abroad.

scholarly journals DEVELOPMENT OF A DRUG BASED ON THE FRUITS OF CHOKEBERRY (ARÓNIA MELANOCÁRPA (MICHX.) EL-LIOT) IMPROVING THE EFFICIENCY OF CANCER CHEMOTHERAPY

2020 ◽  
pp. 219-226
Author(s):  
Valeriya Yur'yevna Andreyeva ◽  
Vladimir Viktorovich Sheykin ◽  
Galina Il'inichna Kalinkina ◽  
Tat'yana Georgiyevna Razina ◽  
Yelena Petrovna Zuyeva ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Raw Materials ◽  
Combined Treatment ◽  
Latin Square ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
New Drugs ◽  
Raw Material ◽  
Black Chokeberry ◽  
Active Substances

Black chokeberry is an official drug raw material and is used as a multivitamin drug. Black chokeberry guarantees the supply of raw materials as it grows all over the Russian Federation end is a promising sourse of phenolic compounds for new drugs. Objective: to develop the most favorable conditions for extraction of bioactive compounds from black chokeberry and to assess its anti-metastatic activity. To extract bioactive compounds from black chokeberry the method of multistep repercolation with completed cycle was used. To assess the factors controlling the raw material extraction the technique of mathematic simulation for latin square. The technique of liquid anthocyanins and catechins rich black chokeberry extraction was given with the following parameters: extragent – 95% acidified alcohol, phase relation – 1 : 5, number of percolators – 5. The content of biologically active substances in the extract obtained with 95% acidified ethyl alcohol was determined by conventional methods. In the composition of the extract, the content of anthocyanins (5.83±0.25%), catechins (0.22±0.02%), tannins (4.65±0.30%), phenolic acids (0.27±0.01%) and other biologically active substances was determined. To assess the antitumor properties of the chokeberry fruit extract, the Lewis lung carcinoma model was used. It was found that the proposed extract reliably inhibits the development of metastases and increases the antimetastatic activity of cyclophosphamide in combined treatment, is of interest as a means for increasing the effectiveness of tumor chemotherapy.

scholarly journals Comparative study of phenolic compounds of the herb of Betonica L. genus species of flora of Ukraine

2021 ◽  
pp. 66-75
Author(s):  
Iryna Sas ◽  
Andrii Hrytsyk ◽  
Taras Koliadzhyn ◽  
Oleh Koshovyi
Keyword(s):  
Phenolic Compounds ◽  
Comparative Study ◽  
Hydroxycinnamic Acids ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
New Drugs ◽  
Raw Material ◽  
Wide Range ◽  
Nitrogen Containing Compounds ◽  
Active Substances

Species of Betonica L. genus are widespread in Ukraine and contain different groups of biologically active substances: hydroxycinnamic acids, flavonoids, tannins, iridoids, terpenoids, steroids, essential oil, organic acids, vitamin K, nitrogen-containing compounds, phenylethanoid glycosides. Species of Betonica L. genus show a wide range of pharmacological activity (anti-inflammatory, antioxidant, choleretic, diuretic, sedative, antitumor, antihypertensive, etc.) and phenolic compounds are one of the most important and promising groups of biologically active substances of these plants. The aim. The aim of the work was to conduct a comparative study of the phenolic compounds of the herb of Betonica L. genus species of flora of Ukraine. Materials and methods. The object of the study was the herb of Betonica peraucta and Betonica brachydonta harvested in the phase of mass flowering of the plant in Ivano-Frankivsk region. The study of phenolic compounds was carried out by paper chromatography, HPLC and spectrophotometry. Results. 7 components of tannins, 4 flavonoids, 5 hydroxycinnamic acids, 2 coumarins were identified and quantified by HPLC in the studied raw material. The quantitative content of the main groups of phenolic compounds in the herb of Betonica peraucta and Betonica brachydonta was determined by the method of absorption spectrophotometry: polyphenols – 5.96 % and 4.82 %, tannins – 1.62 % and 0.68 %, flavonoids – 2.07 % and 1.13 %, hydroxycinnamic acids – 7.01 % and 3.58 %, respectively. Conclusions. As a result of the conducted studies it was found that the content of phenolic compounds in the herb of Betonica peraucta is significantly higher than in the herb of Betonica brachydonta. Therefore, this species is promising for further research and creation of new drugs

Dimeric Drugs

2021 ◽  
Vol 28 ◽  
Author(s):  
Abraham Nudelman
Keyword(s):  
Anticancer Agents ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Active Compounds ◽  
Aids Drugs ◽  
Number Of Classes ◽  
Statistical Effects ◽  
Active Substances

This review intends to summarize the structures of an extensive number of symmetrical-dimeric drugs, having two monomers linked via a bridging entity while emphasizing the large versatility of biologically active substances reported to possess dimeric structures. The largest number of classes of these compounds consist of anticancer agents, antibiotics/antimicrobials, and anti-AIDS drugs. Other symmetrical-dimeric drugs include antidiabetics, antidepressants, analgesics, anti-inflammatories, drugs for the treatment of Alzheimer’s disease, anticholesterolemics, estrogenics, antioxidants, enzyme inhibitors, anti-Parkisonians, laxatives, antiallergy compounds, cannabinoids, etc. Most of the articles reviewed do not compare the activity/potency of the dimers to that of their corresponding monomers. Only in limited cases, various suggestions have been made to justify unexpected higher activity of the dimers vs. the corresponding monomers. These suggestions include statistical effects, the presence of dimeric receptors, binding of a dimer to two receptors simultaneously, and others. It is virtually impossible to predict which dimers will be preferable to their respective monomers, or which linking bridges will lead to the most active compounds. It is expected that the extensive number of articles summarized, and the large variety of substances mentioned, which display various biological activities, should be of interest to many academic and industrial medicinal chemists.

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