scholarly journals Applications of Radiolabelled Curcumin and Its Derivatives in Medicinal Chemistry

2021 ◽  
Vol 22 (14) ◽  
pp. 7410
Author(s):  
Matteo Mari ◽  
Debora Carrozza ◽  
Erika Ferrari ◽  
Mattia Asti
Keyword(s):  
Nuclear Medicine ◽  
Early Diagnosis ◽  
Clinical Application ◽  
Medicinal Chemistry ◽  
Biological Properties ◽  
Present Review ◽  
Chemical Modifications ◽  
Technetium 99M ◽  
Curcumin Derivatives ◽  
Gallium 68

Curcumin is a natural occurring molecule that has aroused much interest among researchers over the years due to its pleiotropic set of biological properties. In the nuclear medicine field, radiolabelled curcumin and curcumin derivatives have been studied as potential radiotracers for the early diagnosis of Alzheimer’s disease and cancer. In the present review, the synthetic pathways, labelling methods and the preclinical investigations involving these radioactive compounds are treated. The studies entailed chemical modifications for enhancing curcumin stability, as well as its functionalisation for the labelling with several radiohalogens or metal radionuclides (fluorine-18, technetium-99m, gallium-68, etc.). Although some drawbacks have yet to be addressed, and none of the radiolabelled curcuminoids have so far achieved clinical application, the studies performed hitherto provide useful insights and lay the foundation for further developments.

Approaches for the synthesis, chemical modification and biological properties of N-acylphenothiazines

2021 ◽  
Vol 10 (4) ◽  
pp. 377-392 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Yulia Matiichuk ◽  
Mohammad Arshad ◽  
Vasyl Matiychuk
Keyword(s):  
Experimental Data ◽  
Chemical Modification ◽  
Medicinal Chemistry ◽  
Biological Properties ◽  
Chemotherapeutic Agents ◽  
Present Review ◽  
The Novel ◽  
Pharmacological Activities ◽  
The Past ◽  
Biological Potential

In this review we systematized the theoretical and experimental data concerning the versatile approaches for the synthesis of N-acylphenothiazines. The aim of the study was to compile the literature reported worldwide in the past 20 years. This article also reviewed the analysis of pharmacological activities of these heterocycles as one of the promising chemotherapeutic objects for the modern bioorganic and medicinal chemistry. It has been hypothesized that the enormous biological potential of these moieties is due to the radical nature in the acyl moiety. Therefore, the present review will be a good contribution to the literature and will provide the platform for the medicinal chemistry researchers to carry out more studies aiming the N-acylphenothiazine moieties as the novel chemotherapeutic agents.

scholarly journals Radionuclidic generators for the production of technetium-99m and rhenium-188

2002 ◽  
Vol 2 (4) ◽  
pp. 235-243 ◽  
Author(s):  
Jurij Vucina ◽  
Dragoljub Lukic
Keyword(s):  
Nuclear Medicine ◽  
Human Body ◽  
Biological Properties ◽  
High Quality ◽  
Technetium 99M ◽  
Physical Chemical ◽  
Low Costs ◽  
99Mtc Generators ◽  
Simple Production ◽  
Therapeutic Nuclear Medicine

The paper deals with production and application of open radioactive sources in modern diagnostic and therapeutic nuclear medicine. In principle, besides adequate physical, chemical and biological properties a reliable route for the routine production of both radionuclide and radiopharmaceutical should be on disposal. The favorite route are radionuclidic generators as they enable simple production of shorter-lived radionuclides at relatively low costs. The main radionuclide in diagnosis is technetium-99m. Its advantages are favorable nuclear properties, availability of large activities of high quality 99mTc at reasonable prices by using (n,f)99Mo/99mTc generators and versatile chemistry. It is used in the investigation of practically all organs and tissues in the human body. Among the betaemitters the radionuclides of rhenium have been recently proposed as suitable candidates for therapeutic applications. The most important is 188Re which is obtained from 188W/188Re generator. Some of the important radiopharmaceuticals labeled with rhenium radionuclides used for certain specific indications are also shown. The activities performed in the Laboratory for Radioisotopes (Vinca Institute of Nuclear Sciences) are also enclosed.

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

Therapeutic Journey of 5-Pyrazolones as a Versatile Scaffold: A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Ravinder Sharma ◽  
Pooja A. Chawla ◽  
Viney Chawla ◽  
Rajeev Verma ◽  
Nandita Nawal ◽  
...  
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Protease Inhibitor ◽  
Medicinal Chemistry ◽  
Membered Ring ◽  
Present Review ◽  
Biological Profile ◽  
3C Protease ◽  
Structure Activity ◽  
Derivatives Of ◽  
Heterocyclic Moiety

Abstract: A sizeable proportion of currently marketed drugs come from heterocycles. The heterocyclic moiety 5-pyrazolone is well known five membered ring containing nitrogen. Derivatives of this wonder nucleus have exhibited activities as diverse as antimicrobial, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antidiabetic, antihyperlipidemic, antiviral, antitubercular, antioxidant, anticancer and antiviral including action against severe acute respiratory syndrome (SARS) or 3C protease inhibitor. A number of drugs based on this motif have already made it to the market. Standard texts and literature on medicinal chemistry cite different approaches for the synthesis of 5-pyrazolones. The present review provides an insight view to 5-pyrazolone synthesis, their biological profile and structure activity relationship studies.

scholarly journals Antiviral Activity of Carrageenans and Processing Implications

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 437
Author(s):  
Milena Álvarez-Viñas ◽  
Sandra Souto ◽  
Noelia Flórez-Fernández ◽  
Maria Dolores Torres ◽  
Isabel Bandín ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Antiviral Activity ◽  
Drug Delivery Systems ◽  
Biological Properties ◽  
Red Seaweed ◽  
Processing Conditions ◽  
Chemical Modifications ◽  
Viral Attachment ◽  
Extraction Stage ◽  
Composition Structure

Carrageenan and carrageenan oligosaccharides are red seaweed sulfated carbohydrates with well-known antiviral properties, mainly through the blocking of the viral attachment stage. They also exhibit other interesting biological properties and can be used to prepare different drug delivery systems for controlled administration. The most active forms are λ-, ι-, and κ-carrageenans, the degree and sulfation position being determined in their properties. They can be obtained from sustainable worldwide available resources and the influence of manufacturing on composition, structure, and antiviral properties should be considered. This review presents a survey of the antiviral properties of carrageenan in relation to the processing conditions, particularly those assisted by intensification technologies during the extraction stage, and discusses the possibility of further chemical modifications.

scholarly journals Evaluation of the effect of an extract of sabugueiro (Sambucus australis) on the labeling of blood constituents with technetium-99m

2007 ◽  
Vol 50 (spe) ◽  
pp. 161-166
Author(s):  
Camila Godinho Ribeiro ◽  
Bernardo Machado Rebello ◽  
Rosane de Figueiredo Neves ◽  
Sebastião David Santos-Filho ◽  
Adenilson de Souza da Fonseca ◽  
...  
Keyword(s):  
Nuclear Medicine ◽  
Blood Cells ◽  
Trichloroacetic Acid ◽  
Wistar Rats ◽  
Blood Samples ◽  
Chemical Substances ◽  
Blood Constituents ◽  
Technetium 99M

Sambucus australis (sabugueiro) has been used to treat inflammatory and rheumatologic disorders. Blood constituents labeled with technetium-99m (99mTc) have been used in nuclear medicine to obtain diagnostic images. The aim of this work was to evaluate the effect of a sabugueiro extract on the labeling of blood cells with 99mTc. Blood samples from Wistar rats were incubated with sabugueiro extract and the radiolabeling assay of blood constituents was carried out. After centrifugation, samples of plasma and blood cells were separated. Aliquots of plasma and blood cells were precipitated with trichloroacetic acid and centrifuged to isolate soluble and insoluble fractions. The radioactivity in each fraction was counted and the percentage of activity (%ATI) was determined. Incubation with sabugueiro extract altered significantly (p<0.05) the %ATI incorporated to the blood constituents. These results could be explained due the presence of chemical substances in the sabugueiro extract that present redox and/or chelating action altering the labeling of the blood constituents with 99mTc.

scholarly journals Infection imaging with radiopharmaceuticals in the 21st century

2002 ◽  
Vol 45 (spe) ◽  
pp. 25-37 ◽  
Author(s):  
Satya S. Das ◽  
Anne V. Hall ◽  
David W. Wareham ◽  
Keith E. Britton
Keyword(s):  
Nuclear Medicine ◽  
Early Diagnosis ◽  
Septic Arthritis ◽  
21St Century ◽  
Recent Trend ◽  
Current Approach ◽  
Infection Imaging ◽  
Prosthetic Devices ◽  
Future Direction ◽  
Diagnosis Of Infection

Infection continues to be a major cause of morbidity and mortality worldwide. Nuclear medicine has an important role in aiding the diagnosis of particularly deep-seated infections such as abscesses, osteomyelitis, septic arthritis, endocarditis, and infections of prosthetic devices. Established techniques such as radiolabelled leucocytes are sensitive and specific for inflammation but do not distinguish between infective and non-infective inflammation. The challenge for Nuclear medicine in infection imaging in the 21st century is to build on the recent trend towards the development of more infection specific radiopharmaceuticals, such as radiolabelled anti-infectives (e.g. 99mTc- ciprofloxacin). In addition to aiding early diagnosis of infection, through serial imaging these agents might prove very useful in monitoring the response to and determining the optimum duration of anti-infective therapy. This article reviews the current approach to infection imaging with radiopharmaceuticals and the future direction it might take.

scholarly journals Technetium-99m nitrido radiopharmaceuticals with unprecedented biological properties

2002 ◽  
Vol 45 (spe) ◽  
pp. 135-142 ◽  
Author(s):  
Adriano Duatti ◽  
Alessandra Boschi ◽  
Licia Uccelli
Keyword(s):  
Perfusion Imaging ◽  
Short Review ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Chemical Methods ◽  
Efficient Tool ◽  
Technetium 99M ◽  
Heart Perfusion ◽  
Diagnostic Agents ◽  
Perfusion Tracer

The chemical methods for the production of technetium-99m radiopharmaceuticals containing a terminal Tc<FONT FACE=Symbol>º</FONT>N triple bond have been established more than a decade ago. From that time, the chemistry of nitrido Tc-99m complexes has provided a highly efficient tool for the design and preparation of novel classes of diagnostic agents, and a number of potentially useful radiopharmaceuticals have been discovered. In particular, nitrido technetium-99m tracers have been developed for heart perfusion imaging. In this short review, the chemical and biological properties of the neutral myocardial perfusion tracer bis(N-ethoxy, N-ethyl-dithiocarbamato) nitrido Tc-99m (TcN-NOEt) will be summarized along with the preparation and preliminary biological evaluation of the first class of monocationic nitrido technetium-99m radiopharmaceuticals exhibiting improved biodistribution properties closer to those expected for an ideal perfusion imaging agent.

Chelators and metal complex stability for radiopharmaceutical applications

2019 ◽  
Vol 107 (9-11) ◽  
pp. 1087-1120 ◽  
Author(s):  
Nkemakonam C. Okoye ◽  
Jakob E. Baumeister ◽  
Firouzeh Najafi Khosroshahi ◽  
Heather M. Hennkens ◽  
Silvia S. Jurisson
Keyword(s):  
Nuclear Medicine ◽  
Metal Complex ◽  
Complex Stability ◽  
Critical Aspect ◽  
Technetium 99M ◽  
Diagnostic Nuclear Medicine ◽  
Key Factor ◽  
The 1960S ◽  
Therapeutic Nuclear Medicine

Abstract Diagnostic and therapeutic nuclear medicine relies heavily on radiometal nuclides. The most widely used and well-known radionuclide is technetium-99m (99mTc), which has dominated diagnostic nuclear medicine since the advent of the 99Mo/99mTc generator in the 1960s. Since that time, many more radiometals have been developed and incorporated into potential radiopharmaceuticals. One critical aspect of radiometal-containing radiopharmaceuticals is their stability under in vivo conditions. The chelator that is coordinated to the radiometal is a key factor in determining radiometal complex stability. The chelators that have shown the most promise and are under investigation in the development of diagnostic and therapeutic radiopharmaceuticals over the last 5 years are discussed in this review.

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