Single Heterocyclic Compounds as Monoamine Oxidase Inhibitors: From Past to Present

2020 ◽  
Vol 20 (10) ◽  
pp. 908-920 ◽  
Author(s):  
Su-Min Wu ◽  
Xiao-Yang Qiu ◽  
Shu-Juan Liu ◽  
Juan Sun
Keyword(s):  
Monoamine Oxidase ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
The Past ◽  
Structure Activity ◽  
Receptor Interactions ◽  
Heterocyclic Derivatives ◽  
Inhibitory Activities ◽  
Leading Compounds ◽  
Heterocyclic Moiety

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson’s disease and Alzheimer’s disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure- activity relationship to provide better correlation among different structures and their receptor interactions.

scholarly journals Chemistry, synthesis and progress report on biological activities of thiadiazole compounds - a review

2016 ◽  
Vol 5 (5) ◽  
pp. 568-588
Author(s):  
Mohammad Asif
Keyword(s):  
Heterocyclic Compounds ◽  
Chelating Agents ◽  
Biological Activities ◽  
Progress Report ◽  
Biological Applications ◽  
Efficacy And Safety ◽  
Metal Chelating ◽  
Structure Activity ◽  
Oxidation Inhibitors ◽  
Relationship Of

Thiadiazoles are an important class of heterocyclic compounds that exhibit diverse applications in organic synthesis, pharmaceutical and biological applications. They are also useful as oxidation inhibitors, cyanine dyes, metal chelating agents, anti-corrosion agents. Researchers across the globe are working on this moiety due to their broad spectrum of applications of thiadiazole chemistry. This article provides information about developments, exploration, synthetic strategies, techniques for the synthesis of thiadiazoles and their diverse biological activities, structure-activity relationship of the compounds and physical properties. This article is an important tool for organic and medicinal chemists to develop newer thiadiazole compounds that could be better agents in terms of efficacy and safety.

scholarly journals Synthesis of Multi-Substituted Pyrrole Derivatives Through [3+2] Cycloaddition with Tosylmethyl Isocyanides (TosMICs) and Electron-Deficient Compounds

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2666 ◽  
Author(s):  
Zhengning Ma ◽  
Zicheng Ma ◽  
Dawei Zhang
Keyword(s):  
Natural Product ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Cycloaddition Reaction ◽  
Synthesis Methods ◽  
Pyrrole Derivatives ◽  
The Past ◽  
Different Types ◽  
Product Structures ◽  
Core Framework

Pyrrole and its polysubstituted derivatives are important five-membered heterocyclic compounds, which exist alone or as a core framework in many pharmaceutical and natural product structures, some of which have good biological activities. The Van Leusen [3+2] cycloaddition reaction based on tosylmethyl isocyanides (TosMICs) and electron-deficient compounds as a substrate, which has been continuously developed due to its advantages such as operationally simple, easily available starting materials, and broadly range of substrates, is one of the most convenient methods to synthetize pyrrole heterocycles. In this review, we discuss the different types of two carbon synthons in the Van Leusen pyrrole reaction and give a summary of the progress of these synthesis methods in the past two decades.

Aurones as New Porcine Pancreatic α-Amylase Inhibitors

2019 ◽  
Vol 16 (3) ◽  
pp. 333-340
Author(s):  
Khashayar Roshanzamir ◽  
Elaheh Kashani-Amin ◽  
Azadeh Ebrahim-Habibi ◽  
Latifeh Navidpour
Keyword(s):  
Biological Activities ◽  
Structural Isomers ◽  
Structural Requirements ◽  
Oh Groups ◽  
Structure Activity ◽  
Inhibitory Activities ◽  
Pharmacological Potential ◽  
Relationship Of ◽  
Amylase Inhibitors

Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturallyoccurring structural isomers of flavones, with promising pharmacological potential. </P><P> Methods: In this study, the structural requirements for the inhibition of porcine pancreatic &#945;- amylase by hydroxylated or methoxylated aurone derivatives were investigated by assessing their in vitro biological activities against porcine pancreatic &#945;-amylase. </P><P> Results: The structure-activity relationship of these inhibitors based on both in vitro and in silico findings showed that the hydrogen bonds between the OH groups of the A or B ring of (Z)- benzylidenebenzofuran-3-one derivatives and the catalytic residues of the binding site are crucial for their inhibitory activities. </P><P> Conclusion: It seems that the OH groups in aurones inhibit &#945;-amylase in a manner similar to that of OH groups in flavones and flavonols.

Bioactive Heterocyclic Compounds as Potential Therapeutics in the Treatment of Gliomas: A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Reyaz Hassan ◽  
Roohi Mohi-ud-din ◽  
Mohammad Ovais Dar ◽  
Abdul Jalil Shah ◽  
Prince Ahad Mir ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Anticancer Activities ◽  
Tumour Heterogeneity ◽  
Cancer Cell Death ◽  
Wide Range ◽  
Heterocyclic Derivatives ◽  
Current Therapies ◽  
Terminal Prognosis ◽  
Potential Therapeutics

: Cancer is one of the most alarming diseases, with an estimation of 9.6 million deaths in 2018. Glioma occurs in glial cells surrounding nerve cells. The majority of the patients with gliomas have a terminal prognosis, and the ailment has significant sway on patients and their families, be it physical, psychological, or economic wellbeing. As Glioma exhibits, both intra and inter tumour heterogeneity with multidrug resistance and current therapies are ineffective. So the development of safer anti gliomas agents is the need of hour. Bioactive heterocyclic compounds, eithernatural or synthetic,are of potential interest since they have been active against different targets with a wide range of biological activities, including anticancer activities. In addition, they can cross the biological barriers and thus interfere with various signalling pathways to induce cancer cell death. All these advantages make bioactive natural compounds prospective candidates in the management of glioma. In this review, we assessed various bioactive heterocyclic compounds, such as jaceosidin, hispudlin, luteolin, silibinin, cannabidiol, tetrahydrocannabinol, didemnin B, thymoquinone, paclitaxel, doxorubicin, and cucurbitacins for their potential anti-glioma activity. Also, different kinds of chemical reactions to obtain various heterocyclic derivatives, e.g. indole, indazole, benzimidazole, benzoquinone, quinoline, quinazoline, pyrimidine, and triazine, are listed.

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 Synthetic and therapeutic potential of 4-thiazolidinone and its analogs

2021 ◽  
pp. 119-138 ◽  
Author(s):  
Neetu Agrawal
Keyword(s):  
Therapeutic Agent ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
The Past ◽  
Structure Activity ◽  
Potent Therapeutic Agent

Past researches on 4-thiazolidinone nucleus have revealed the prominent potential of derivatives containing this nucleus to be developed as a potent therapeutic agent. Because of these biological activities, their structure-activity relationship has created an interest for medicinal chemists leading to the discovery of a number of lead molecules. This review highlights the routes for its synthesis and summarizes the past and recent studies on its biological activities to guide the medicinal chemists working on this nucleus in the development of clinically viable drugs.

scholarly journals A review on heterocyclic moieties and their applications

2016 ◽  
Vol 2 (1) ◽  
pp. 99-115
Author(s):  
Syed Sabir ◽  
Mansour Ibrahim Alhazza ◽  
Ahmed Aidid Ibrahim
Keyword(s):  
Present Article ◽  
Heterocyclic Compounds ◽  
Corrosion Inhibitors ◽  
Antimicrobial Agents ◽  
State Of The Art ◽  
Synthesis Methods ◽  
Wide Range ◽  
Heterocyclic Derivatives ◽  
Synthesis Reactions ◽  
Heterocyclic Moiety

AbstractSeveral described in literature crosslinking methods to obtain heterocyclic moieties were discussed in this review. Selected important properties of polyamides and their synthesis reactions were briefly presented. The heterocyclic moieties displayed a wide range of applications in medicine and industry. New heterocyclic derivatives obtained by linking heterocyclic moiety to amic acids and imides found diverse applications: as surfactants, antimicrobial agents, or corrosion inhibitors. The present article describes the state-of-the art synthesis methods of the heterocyclic compounds and their application.

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