scholarly journals The synthesis of angular heteroarenochromones based on 7-hydroxy-8-carbonylchromones

2017 ◽  
Vol 5 (2) ◽  
pp. 68-94 ◽  
Author(s):  
Tatyana Shokol ◽  
Oleg Lozinski ◽  
Natalia Gorbulenko ◽  
Volodymyr Khilya

The present review highlights advanced strategies to the synthesis of the chromones annulated with O- and N-containing heterocycles at C(7)-C(8) bond. Due to the prevalence of such motives in different kinds of natural flavonoids and some alkaloids, fused chromones have attracted a great deal of attention so far. On the other hand a wide range of biological activities is displayed by the compounds of this type both among naturally occurring flavonoids and their synthetic analogues. 8-Carbonyl-7-hydroxychromones proved to be versatile synthones for the synthesis of angular hetarenochromones via approach of annulation of a heterocycle to the chromone core. It also addresses the question of the biological activity of naturally occurring and fused synthetic hetarenochromones.

2021 ◽  
Vol 31 (1) ◽  
Author(s):  
Waill A. Elkhateeb ◽  
Kareem M. Mousa ◽  
Marwa O. ELnahas ◽  
Ghoson M. Daba

Abstract Background Biological control of insects is the current goal of modern researches to avoid using the harmful chemicals. Some fungi are capable of infecting and killing insects and, hence, are commonly known as entomopathogenic fungi (EPF). On the other hand, some insects can kill harmful fungal strains using their products such as peptides. Hence, the aim of this review article is to highlight the use of EPF as biocontrol tools against each other. Results EPF are generally characterized by having a wide range of hosts which made them the perfect candidate for biological control missions. They are existing in abundance in the environment and involved in plenty of environmental interactions. They have prestigious enzymatic machinery and toxins that contribute as killing tools. Moreover, after penetrating the insect, the expanded vegetative growth of hyphal bodies enabling the invasion of the fungi throughout the entire tissues of host insect cause physic, histolytic, and pathologic changes ultimately leading to the death of the host insect. On the other hand, some insects can kill harmful fungal strains using their secreted products such as peptides. Conclusion In this review, the use of fungi and insects as biological control agents against each other was described. Furthermore, the history of using EPF for this purpose, their killing mechanism, host range, and the factors affecting EPF virulence were highlighted. Moreover, the role of insect’s immunology and some insect’s products as antifungal agents was presented focusing on peptides with biological activities against fungi. Finally, future prospects concerning the use of insects and fungi in biological control process were discussed.


Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 791 ◽  
Author(s):  
Carla Fernandes ◽  
Maria Carraro ◽  
João Ribeiro ◽  
Joana Araújo ◽  
Maria Tiritan ◽  
...  

Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest in synthetic chiral derivatives of xanthones (CDXs) has been witnessed. The synthetic methodologies can afford structures that otherwise could not be reached within the natural products for biological activity and SAR studies. Another reason that justifies this trend is that both enantiomers can be obtained by using appropriate synthetic pathways, allowing the possibility to perform enantioselectivity studies. In this work, a literature review of synthetic CDXs is presented. The structures, the approaches used for their synthesis and the biological activities are described, emphasizing the enantioselectivity studies.


2018 ◽  
Vol 13 (3) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Serhat S. Çiçek ◽  
Sara Vitalini ◽  
Christian Zidorn

The present review gives an overview about naturally occurring phenyldihydroisocoumarins, their sources, and bioactivities. In total, 54 compounds are covered, including eight substances which are in fact alkaloids or protoalkaloids. These nitrogen containing compounds were exclusively found in the Papaveraceae family. The remaining 46 compounds have been reported from twelve different source families, ranging from mosses to angiosperms. Six of the nitrogen free compounds feature additional rings, while 40 are simple phenyldihydroisocoumarins with substituents in all possible positions, except 3, 2’, and 6’. Common substituents of these simple phenyldihydroisocoumarins are hydroxy groups, methoxy groups, and glucosyloxy groups; on the other hand, acuminosyloxy and rutinosyloxy groups have so far been found only in one and two naturally occurring phenyldihydroisocoumarins, respectively. Though a number of bioactivities have been proven for phenyldihydroisocoumarins, ranging from anticancer and antidiabetic to antimicrobial and anti-inflammatory activities, so far only one taxon, Hydrangea macrophylla var. thunbergii, is widely used. Moreover, the usage of this taxon is mainly due to the sweet taste properties of the contained phenyldihydroisocoumarin phyllodulcin and less based on the alleged health-promoting effects of its constituents.


Author(s):  
Abhinav Anand ◽  
Neha Sharma ◽  
Navneet Khurana

Objective: To predict the biological activity of certain phytoconstituents for their anti-AD effects.Methods: Several phytoconstituents were selected on the basis of reported literature. The anti-AD activities of selected phytoconstituents were predicted by employing canonical simplified molecular-input line-entry system obtained from PubChem using PASS online.Results: Several phytoconstituents were predicted to have effects better than marketed drugs under some or the other out of the chosen six areas of pharmacological intervention. On the other hand, several new avenues were predicted in which the in vitro and in vivo evaluation of the phytoconstituents can be made on the basis of PASS predicted activities.Conclusion: PASS is an important tool for virtually screening the compounds of interest for the biological activities of interest. This helps the researchers to streamline the research. However, PASS has its own share of limitations amidst a multitude of merits.


2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.


2020 ◽  
Vol 20 (19) ◽  
pp. 2019-2035
Author(s):  
Esmaeil Sheikh Ahmadi ◽  
Amir Tajbakhsh ◽  
Milad Iranshahy ◽  
Javad Asili ◽  
Nadine Kretschmer ◽  
...  

Naturally occurring naphthoquinones (NQs) comprising highly reactive small molecules are the subject of increasing attention due to their promising biological activities such as antioxidant, antimicrobial, apoptosis-inducing activities, and especially anticancer activity. Lapachol, lapachone, and napabucasin belong to the NQs and are in phase II clinical trials for the treatment of many cancers. This review aims to provide a comprehensive and updated overview on the biological activities of several new NQs isolated from different species of plants reported from January 2013 to January 2020, their potential therapeutic applications and their clinical significance.


2020 ◽  
Vol 20 (14) ◽  
pp. 1310-1323
Author(s):  
Andrea Bosso ◽  
Antimo Di Maro ◽  
Valeria Cafaro ◽  
Alberto Di Donato ◽  
Eugenio Notomista ◽  
...  

Host defence peptides (HDPs) are powerful modulators of cellular responses to various types of insults caused by pathogen agents. To date, a wide range of HDPs, from species of different kingdoms including bacteria, plant and animal with extreme diversity in structure and biological activity, have been described. Apart from a limited number of peptides ribosomally synthesized, a large number of promising and multifunctional HDPs have been identified within protein precursors, with properties not necessarily related to innate immunity, consolidating the fascinating hypothesis that proteins have a second or even multiple biological mission in the form of one or more bio-active peptides. Among these precursors, enzymes constitute certainly an interesting group, because most of them are mainly globular and characterized by a fine specific internal structure closely related to their catalytic properties and also because they are yet little considered as potential HDP releasing proteins. In this regard, the main aim of the present review is to describe a panel of HDPs, identified in all canonical classes of enzymes, and to provide a detailed description on hydrolases and their corresponding HDPs, as there seems to exist a striking link between these structurally sophisticated catalysts and their high content in cationic and amphipathic cryptic peptides.


2020 ◽  
pp. 004051752092551
Author(s):  
Javeed A Awan ◽  
Saif Ur Rehman ◽  
Muhammad Kashif Bangash ◽  
Fiaz Hussain ◽  
Jean-Noël Jaubert

Curcumin is a naturally occurring hydrophobic polyphenol compound. It exhibits a wide range of biological activities such as antibacterial, anti-inflammatory, anti-carcinogenic, antifungal, anti-HIV, and antimicrobial activity. In this research work, antimicrobial curcumin nanofibrous membranes are produce by an electrospinning technique using the Eudragit RS 100 (C19H34ClNO6) polymer solution enriched with curcumin. The morphology and chemistry of the membrane are analyzed using scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Kirby Bauer disk diffusion tests are carried out to examine the antibacterial effectiveness of the membrane. Experimental results show that the nanofibers produced are of uniform thickness morphology and curcumin is successfully incorporated into the nanofibrous mat, while no chemical bonding was observed between curcumin and the polymer. The antimicrobial curcumin nanofibrous membranes can be effectively applied as antimicrobial barrier in a wide variety of medical applications such as wound healing, scaffolds, and tissue engineering.


1989 ◽  
Vol 67 (8) ◽  
pp. 1354-1358 ◽  
Author(s):  
Jacques Paquet ◽  
Paul Brassard

The behaviour of various types of polar dienes towards halogenated ortho quinones has been investigated in a number of representative cases. As compared to the commonly used para analogues, o-quinones provide a wide range of products that indicate a keener response to the nature, number, and position of substituents on both reactants. 3-Halogenated-o-naphthoquinones 1 and 2 react smoothly with a representative vinologous ketene acetal 3, vinylketene acetals 4 and 5, and a monooxygenated diene 6 to provide variously substituted phenanthrenequinones 7–11. Only monooxygenated dienes on the other hand add to o-benzoquinones 14–16 and give convenient syntheses of the corresponding o-naphthoquinones 18–20. Keywords: cycloaddition, o-naphthoquinones, phenanthrenequinones, regiospecificity.


2002 ◽  
Vol 55 (1) ◽  
pp. 1-37 ◽  
Author(s):  
Craig A. Monson

Abstract Reexamination of a wide range of documents surrounding the twenty-second, twenty-fourth, and twenty-fifth sessions of the Council of Trent reveals that delegates strived officially to say as little as possible about music: only that secular or impure elements should be eliminated and that specific issues should be settled locally, by individual bishops and provincial synods. But, beginning with Gustave Reese, several scholars have misleadingly strung together a preliminary canon, stressing textual intelligibility, which was never approved in the general congregations, and the few lines that actually supplanted it, concerned only with the elimination of lasciviousness. On the other hand, a largely unrecognized or misunderstood attack on church polyphony did occur at the less familiar twenty-fifth session, when Gabriele Paleotti may have attempted to suppress elaborate music in female monasteries. Although this attempt was rejected in the general congregations, its restrictions were subsequently revived by local authorities such as Paleotti and Carlo Borromeo in their own dioceses. In the Council's immediate aftermath, reformers such as Paleotti and Borromeo once again focused on the issue of intelligibility, affording it a quasi-official status that seems to have quickly become widely accepted as “iuxta formam concilii.”


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