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.

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.

Recent Advances in Therapeutic Applications of Bisbenzimidazoles

2020 ◽  
Vol 16 (4) ◽  
pp. 454-486 ◽  
Author(s):  
Smita Verma ◽  
Vishnuvardh Ravichandiran ◽  
Nihar Ranjan ◽  
Swaran J.S. Flora
Keyword(s):  
Heterocyclic Compounds ◽  
Wide Spectrum ◽  
Dna Recognition ◽  
Present Review ◽  
Pharmacological Activities ◽  
Structural Motifs ◽  
Therapeutic Applications ◽  
The Past ◽  
Recent Advances

Nitrogen-containing heterocycles are one of the most common structural motifs in approximately 80% of the marketed drugs. Of these, benzimidazoles analogues are known to elicit a wide spectrum of pharmaceutical activities such as anticancer, antibacterial, antiparasitic, antiviral, antifungal as well as chemosensor effect. Based on the benzimidazole core fused heterocyclic compounds, crescent-shaped bisbenzimidazoles were developed which provided an early breakthrough in the sequence-specific DNA recognition. Over the years, a number of functional variations in the bisbenzimidazole core have led to the emergence of their unique properties and established them as versatile ligands against several classes of pathogens. The present review provides an overview of diverse pharmacological activities of the bisbenzimidazole analogues in the past decade with a brief account of its development through the years.

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.

Recent advancements on Benzimidazole: A versatile scaffold in medicinal chemistry

2021 ◽  
Vol 21 ◽  
Author(s):  
Zohor Mohammad Mahdi Alzhrani ◽  
Mohammad Mahboob Alam ◽  
Syed Nazreen
Keyword(s):  
Clinical Trials ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Present Review ◽  
Benzimidazole Derivatives ◽  
The Past ◽  
Anti Inflammatory

: Benzimidazole is nitrogen containing fused heterocycle which has been extensively explored in medicinal chemistry. Benzimidizole nucleus has been found to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, antiviral, antitubercular and antidiabetic. A number of benzimidazoles such as bendamustine, pantoprazole have been approved for the treatment of various illnesses whereas galeterone and GSK461364 are in clinical trials. The present review article gives an overview about the different biological activities exhibited by the benzimidazole derivatives as well as different methods used for the synthesis of benzimidazole derivatives for the past ten years.

Therapeutic Potential of Cinnoline Core: A Comprehensive Review

2020 ◽  
Vol 20 (3) ◽  
pp. 196-218
Author(s):  
Rajiv K. Tonk ◽  
Sandhya Bawa ◽  
Deepak Kumar
Keyword(s):  
Heterocyclic Compounds ◽  
Therapeutic Potential ◽  
Biological Properties ◽  
Present Review ◽  
Natural Occurrence ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Wide Range ◽  
The Family ◽  
Almost All

Cinnoline or Benzo-pyridazine has its place in the family of fairly well-known benzfuseddiazine heterocycles. Because of its natural occurrence and synthetic exploration, cinnoline compounds validated its thought-provoking bioactivity through a number of research publications and patents during last few decades. A creative consideration has been rewarded to the synthesis of cinnoline based heterocyclic compounds, mostly due to their wide range of diverse pharmacological activities. The present review covers the principle approaches to the synthesis of cinnoline nucleus and almost all biological properties of 115 cinnoline derivatives reported during the last 65 years from natural and synthetic origin with 140 references.

Derivatives and Analogues of Resveratrol: Recent Advances in Structural Modification

2019 ◽  
Vol 19 (10) ◽  
pp. 809-825 ◽  
Author(s):  
Qing-Shan Li ◽  
Yao Li ◽  
Girdhar Singh Deora ◽  
Ban-Feng Ruan
Keyword(s):  
Structural Modification ◽  
Biological Activities ◽  
Biological Properties ◽  
Synthetic Analogues ◽  
Pharmacological Activities ◽  
The Past ◽  
Structure Activity ◽  
Clinical Drugs ◽  
New Compounds ◽  
Reliable Basis

Resveratrol is a non-flavonoid polyphenol containing a terpenoid backbone. It has been intensively studied because of its various promising biological properties, such as anticancer, antioxidant, antibacterial, neuroprotective and anti-inflammatory activities. However, the medicinal application of resveratrol is constrained by its poor bioavailability and stability. In the past decade, more attention has been focused on making resveratrol derivatives to improve its pharmacological activities and pharmacokinetics. This review covers the literature published over the past 15 years on synthetic analogues of resveratrol. The emphasis is on the chemistry of new compounds and relevant biological activities along with structure-activity relationship. This review aims to provide a scientific and reliable basis for the development of resveratrol-based clinical drugs.

scholarly journals Medulloblastoma cancer stem cells: molecular signatures and therapeutic targets

2020 ◽  
Vol 73 (5) ◽  
pp. 243-249 ◽  
Author(s):  
Hisham F Bahmad ◽  
Robert J Poppiti
Keyword(s):  
Stem Cells ◽  
Cancer Stem Cells ◽  
Cancer Biology ◽  
Cancer Recurrence ◽  
Chemotherapeutic Agents ◽  
Molecular Signatures ◽  
The Novel ◽  
Therapeutic Approaches ◽  
Successful Management ◽  
The Past

Medulloblastoma (MB) is the most common malignant primary intracranial neoplasm diagnosed in childhood. Although numerous efforts have been made during the past few years to exploit novel targeted therapies for this aggressive neoplasm, there still exist substantial hitches hindering successful management of MB. Lately, progress in cancer biology has shown evidence that a subpopulation of cells within the tumour, namely cancer stem cells (CSCs), are thought to be responsible for the resistance to most chemotherapeutic agents and radiation therapy, accounting for cancer recurrence. Hence, it is crucial to identify the molecular signatures and genetic aberrations that characterise those CSCs and develop therapies that specifically target them. In this review, we aim to give an overview of the main genetic and molecular cues that depict MB-CSCs and provide a synopsis of the novel therapeutic approaches that specifically target this population of cells to attain enhanced antitumorous effects and therefore overcome resistance to therapy.

scholarly journals Importance of Fluorine in Benzazole Compounds

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4677
Author(s):  
Thuraya Al-Harthy ◽  
Wajdi Zoghaib ◽  
Raid Abdel-Jalil
Keyword(s):  
Small Molecules ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Short Review ◽  
Significant Enhancement ◽  
Pharmacological Activities ◽  
The Past ◽  
To Receive

Fluorine-containing heterocycles continue to receive considerable attention due to their unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules imparts a significant enhancement their biological activities compared to non-fluorinated molecules. In this short review, we will highlight the importance of incorporating fluorine as a basic appendage in benzothiazole and benzimidazole skeletons. The chemistry and pharmacological activities of heterocycles containing fluorine during the past years are compiled and discussed.

Exploration of the Biological Potential of Benzoxazoles: An Overview

2019 ◽  
Vol 16 (2) ◽  
pp. 111-126 ◽  
Author(s):  
Mayura Kale ◽  
Vijayalaxmi Chavan
Keyword(s):  
Biological Activities ◽  
Research Work ◽  
Present Review ◽  
Pharmacological Activities ◽  
Biological Potential

The development of benzoxazole containing drugs and research compounds has been discussed in the present review along with its varied pharmacological activities such as antimicrobial, antiinflammatory, anticancer, antiviral, antiasthmatic, antitubercular, anticonvulsant, lipid modulating, anticoagulants, antidiabetic and anthelmintic activities. The present review is a compilation of the biological activities determined in the research work conducted on benzoxazole-based compounds fused and linked with various other heterocycles.

Hydraulic Laboratory at University of Liège

2018 ◽  
pp. 80-89
Author(s):  
Willi H. Hager
Keyword(s):  
Basic Research ◽  
The Novel ◽  
University Campus ◽  
Current Position ◽  
Professional Background ◽  
The Past ◽  
Comprehensive Picture

The Hydraulic Laboratory of Liège University, Belgium, is historically considered from its foundation in 1937 to the mid-1960s. The technical facilities of the various Buildings are highlighted, along with canals and instrumentation available. It is noted that in its initial era, comparatively few basic research has been conducted, mainly due to the professional background of the professors leading the establishment. This state was improved in the past 50 years, however, particularly since the Laboratory was dislocated to its current position in the novel University Campus. Biographies of the leading persons associated with the Liège Hydraulic Laboratory are also presented, so that a comprehensive picture is given of one of the currently leading hydraulic Laboratories of Europe.

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