scholarly journals Synthesis of linear hetarenochromones based on 7-hydroxy-6-formyl(acetyl)chromones

2021 ◽  
Vol 9 (1) ◽  
pp. 70-96
Author(s):  
Tatyana Shokol ◽  
Natalia Gorbulenko ◽  
Khilya Volodymyr

Fused chromones are attracting increasing attention as novel therapeutic agents due to their wide distribution in nature, effective bioactivities and low toxicity. 6-Carbonyl-7-hydroxychromones proved to be versatile synthons for the synthesis of linear hetarenochromones by annulation of heterocycle to the chromone core. The present review is focused on the syntheses of furo[3,2-g]chromones, pyrano[3,2-g]chromones and some of their N-containing analogues, namely chromeno[6,7-d]isoxazoles, pyrano[3’,2’:6,7]chromeno[4,3-b]pyridine-5,11-diones and pyrano[3’,2’:6,7]chromeno[4,3-c]pyridine-5,11-diones based on the 7-hydroxy-6-formylchromones or 7-hydroxy-6-acetylchromones and shows the current state of research to date. The methods for the synthesis of the starting 7-hydroxy-6-formylchromones and 7-hydroxy-6-acetylchromones have been also mentioned. The biological activity of naturally occurring and modified synthetic linear hetarenochromones has been also represented.

2021 ◽  
Vol 37 (2) ◽  
pp. 3-19
Author(s):  
A.A. Gagarina

The present review describes the concept of probiotics for plants and analyzes the prospects for using actinomycetes as producers of these drugs. The minimum requirements for plant probiotic microorganisms are proposed, similar to those for human probiotic microorganisms. These are utility, efficiency and safety for plants, as well as mandatory isolation from plant samples. It is noted that these requirements are usually met by endophytic and rhizosphere microorganisms that stimulate plant growth and provide them with protection from phytopathogens. Evidence is given for the possibility of attributing actinomycetes to probiotic plant bacteria, due to the close relationship of these microorganisms with plants, their wide distribution in populations of endophytic and rhizosphere microorganisms, and the presence of phytoregulatory activity. The review provides examples of genera and species of actinomycetes that are promising producers of probiotics for agronomically important crops. The most studied and commercialized of them are representatives of the Streptomyces genus. The current state, prospects and problems in commercialization of probiotics based on actinomycetes are discussed. probiotic microorganisms of plants, associative actinomycetes, endophytes, rhizosphere, biological preparations


2019 ◽  
Vol 36 (5) ◽  
pp. 753-768 ◽  
Author(s):  
Edward Owen Norman ◽  
James Lever ◽  
Robert Brkljača ◽  
Sylvia Urban

This review provides a summary of the current state of research concerning the unique specialised metabolites from Haemodoraceae.


Author(s):  
Suresh Choudhary ◽  
G Jeyabalan ◽  
Naresh Kalra

The Benzothiazole nucleus is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities, such as antitumor, antimicrobial, anthelmintic, antileishmanial, anticonvulsant and anti-inflammatory. The present review focuses on the benzothiazoles with potential activities that are now in development. The synthesized benzothiazole derivatives could be considered as lead molecule for the development of therapeutic agents.


2019 ◽  
Vol 20 (6) ◽  
pp. 1461 ◽  
Author(s):  
Tomonari Kinoshita ◽  
Taichiro Goto

Idiopathic pulmonary fibrosis (IPF) is defined as a specific form of chronic, progressive fibrosing interstitial pneumonia of unknown cause, occurring primarily in older adults, and limited to the lungs. Despite the increasing research interest in the pathogenesis of IPF, unfavorable survival rates remain associated with this condition. Recently, novel therapeutic agents have been shown to control the progression of IPF. However, these drugs do not improve lung function and have not been tested prospectively in patients with IPF and coexisting lung cancer, which is a common comorbidity of IPF. Optimal management of patients with IPF and lung cancer requires understanding of pathogenic mechanisms and molecular pathways that are common to both diseases. This review article reflects the current state of knowledge regarding the pathogenesis of pulmonary fibrosis and summarizes the pathways that are common to IPF and lung cancer by focusing on the molecular mechanisms.


Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4330
Author(s):  
Ngonidzashe Ruwizhi ◽  
Blessing Atim Aderibigbe

Several researchers have reported the use of cholesterol-based carriers in drug delivery. The presence of cholesterol in cell membranes and its wide distribution in the body has led to it being used in preparing carriers for the delivery of a variety of therapeutic agents such as anticancer, antimalarials and antivirals. These cholesterol-based carriers were designed as micelles, nanoparticles, copolymers, liposomes, etc. and their routes of administration include oral, intravenous and transdermal. The biocompatibility, good bioavailability and biological activity of cholesterol-based carriers make them potent prodrugs. Several in vitro and in vivo studies revealed cholesterol-based carriers potentials in delivering bioactive agents. In this manuscript, a critical review of the efficacy of cholesterol-based carriers is reported.


1982 ◽  
Vol 12 (3) ◽  
pp. 563-573 ◽  
Author(s):  
S. Greer ◽  
Peter M. Silberfarb

SYNOPSISAn increasing interest in the psychological concomitants of neoplastic diseases has led to a burgeoning literature in recent years. The present review identifies five major areas of psychiatric research, documents the current state of knowledge, and indicates fruitful avenues for further study.


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.


2020 ◽  
Vol 128 (6) ◽  
pp. 852
Author(s):  
О.П. Черкасова ◽  
Д.С. Сердюков ◽  
А.С. Ратушняк ◽  
Е.Ф. Немова ◽  
Е.Н. Козлов ◽  
...  

Terahertz (THz) radiation and related technologies are rapidly developed and find their application in different branches of science and technology, including medical diagnostics and therapy. This poses a problem of determining the safety limits of the human body exposure to THz radiation, which is closely related to a problem of biological activity of THz waves. Therefore, in this work, the current state of research in the area of THz radiation – cells interaction is overviewed.


2020 ◽  
Author(s):  
Johnson Olaleye Oladele ◽  
Oyedotun Moses Oyeleke ◽  
Oluwaseun Titilope Oladele ◽  
Boyede Dele Olowookere ◽  
Babatunde Joseph Oso ◽  
...  

Abstract The outbreak of COVID-19 caused by SARS-CoV-2 is increasing with an alarming rate of associated frightening mortality without no known approved therapy. The emergence of new infectious diseases and increase in frequency of drug resistant viruses demand effective and novel therapeutic agents. This study investigated the putative inhibitory potentials of apigenin, fisetin, kolaflavanone, and remdesivir towards SARS-COV2 major protease (6LU7) using in silico methods. Pharmacodynamics, pharmacokinetics and toxicological profiles of the compounds were also examined using the pkCSM server. All the compounds showed good affinity to the binding pocket of 6LU7. It was observed that kolaflavanone exhibited the highest binding affinity when compared to apigenin, fisetin, and remdesivir. The amino acids ASN238, TYR237, LEU286, and LEU287 were showed as the key residues for kolaflavanone binding to human SARS-COV2 major protease. The Pharmacodynamics and pharmacokinetics results suggested that all the tested compounds have significant drug likeness properties and they could be absorbed through the human intestine. Additionally, all the tested compounds except remdesivir are not hepatoxic and also displayed non or relatively low toxic effects in human. Summarily, the results of this study indicated that all the tested compounds are potential putative inhibitors of SARS-COV2 major protease with no or low toxicity effects. However, further experimental and clinical studies are needed to further explore their activities and validate their efficacies against COVID-19.


2016 ◽  
Vol 12 ◽  
pp. 769-795 ◽  
Author(s):  
Daniel Wiegmann ◽  
Stefan Koppermann ◽  
Marius Wirth ◽  
Giuliana Niro ◽  
Kristin Leyerer ◽  
...  

Muraymycins are a promising class of antimicrobial natural products. These uridine-derived nucleoside-peptide antibiotics inhibit the bacterial membrane protein translocase I (MraY), a key enzyme in the intracellular part of peptidoglycan biosynthesis. This review describes the structures of naturally occurring muraymycins, their mode of action, synthetic access to muraymycins and their analogues, some structure–activity relationship (SAR) studies and first insights into muraymycin biosynthesis. It therefore provides an overview on the current state of research, as well as an outlook on possible future developments in this field.


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