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.

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 Biological Potential and Chemical Properties of Pyridine and Piperidine Fused Pyridazine Compounds: Pyridopyridazine a Versatile Nucleus

2016 ◽  
Vol 1 (1) ◽  
pp. 29 ◽  
Author(s):  
Mohammad Asif
Keyword(s):  
Nitrogen Atom ◽  
Structural Feature ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Properties ◽  
Pharmacological Properties ◽  
Drug Molecules ◽  
Biological Potential ◽  
Different Types ◽  
And Chemical Properties

Pyridopyridazine compounds are important nitrogen atom containing heterocyclic compounds due to their pharmacological versatility. This heterocycle system characterized a structural feature for different types of bioactive compounds that exhibiting various types of biological activities which make it an attractive scaffold for the design and development of new drug molecules. This article provided information about the pharmacological properties of pyridopyridazines derivatives.

scholarly journals COMPONENT COMPOSITION AND BIOLOGICAL ACTIVITY OF GENUS VIOLA (VIOLACEAE) OF RUSSIAN FLO-RA

2020 ◽  
pp. 19-45
Author(s):  
Natal'ya Valeriyevna Petrova ◽  
Nina Anatol'yevna Medvedeva
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Component Composition ◽  
The Past ◽  
Aerial Parts ◽  
Different Types ◽  
The Subject ◽  
The Russian Federation ◽  
Chemical Formulas

The subject of the review is the component composition and biological activity of species of genus Viola L. (Violaceae) from the flora of the Russian Federation according publications appeared over the past few decades. Chemical constituents and biological activities have been reported for 24 species of the 100 Viola species occurring in Russian. Components of various structures: flavonoids, cyclotides, anthocyanidins, phenylpropanoic acids, coumarins, alkaloids, fatty acids and its derivatives and ect. were found in the roots, aerial parts, flowers and leaves. Composition of 137 flavonoids, alkaloids, coumarins etc. was expanded with references to their chemical formulas and literature sources. Data of the essential oils isolated from the leaves of V. tricolor L., V. arvensis Murray, V. yedoensis Makino и V. odorata L. is systematized. It was demonstrated that extracts, their fractions, and some components showed different types of biological activity, including anti-inflammatory, cytotoxic and antiviral ones. The revealed range of biological activity partially confirmed expediency of using species of genus Viola in folk and standard practice medicine.

Synthetic Methods and Pharmacological Potential of Different Oxazine Analogs

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran
Keyword(s):  
Organic Chemistry ◽  
Drug Resistance ◽  
Sodium Hydroxide ◽  
Crucial Role ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Wide Range ◽  
Different Types ◽  
Pharmacological Potential

: Oxazine analog is a vital class of heterocyclic compounds and has attracted synthetic interest owing to their wide range of biological activities. Oxazine analogs are valuable in medicinal organic chemistry and exhibited different varieties of biological activities such as antimicrobial, anticancer, antimalarial, antitubercular, sedative, anticonvulsant, analgesic, anti-inflammatory, antipyretic, etc. Oxazine can be derived from benzene by appropriate substitution of carbon atoms of the ring by nitrogen and oxygen atoms. Nowadays, the development of drug resistance is a key problem, and to defeat this problem, it is crucial to synthesize novel compounds. So novel oxazine analogs may play a crucial role to overcome these problems. Oxazine analogs are prepared by reaction of chalcone derivatives with thiourea in the presence of alcohol and sodium hydroxide. The present aims of this review to give an outline of some different synthetic methods and different types of biological activities of oxazine analogs. We hope that this review will be motivating for researchers concerned with oxazine analogs.

scholarly journals A Review on Phytochemicals of the Genus Maytenus and Their Bioactive Studies

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4563
Author(s):  
Yuan-Yuan Huang ◽  
Lu Chen ◽  
Guo-Xu Ma ◽  
Xu-Dong Xu ◽  
Xue-Gong Jia ◽  
...  
Keyword(s):  
Theoretical Basis ◽  
Biological Activities ◽  
Current Status ◽  
Synthesis Methods ◽  
Chemical Research ◽  
Structural Classification ◽  
The Past ◽  
Development And Utilization ◽  
Hiv Inhibition ◽  
New Compounds

The genus Maytenus is a member of the Celastraceae family, of which several species have long been used in traditional medicine. Between 1976 and 2021, nearly 270 new compounds have been isolated and elucidated from the genus Maytenus. Among these, maytansine and its homologues are extremely rare in nature. Owing to its unique skeleton and remarkable bioactivities, maytansine has attracted many synthetic endeavors in order to construct its core structure. In this paper, the current status of the past 45 years of research on Maytenus, with respect to its chemical and biological activities are discussed. The chemical research includes its structural classification into triterpenoids, sesquiterpenes and alkaloids, along with several chemical synthesis methods of maytansine or maytansine fragments. The biological activity research includes activities, such as anti-tumor, anti-bacterial and anti-inflammatory activities, as well as HIV inhibition, which can provide a theoretical basis for the better development and utilization of the Maytenus.

Some applications of deep eutectic solvents in alkylation of heterocyclic compounds: A review of the past 10 years

2021 ◽  
Vol 27 (1) ◽  
pp. 45-56
Author(s):  
Maja Molnar ◽  
Melita Lončarić ◽  
Martina Jakovljević ◽  
Mario Komar ◽  
Mirjana Lončar
Keyword(s):  
Green Chemistry ◽  
Heterocyclic Compounds ◽  
Deep Eutectic Solvents ◽  
The Past ◽  
Different Types ◽  
Insight Into

AbstractThis mini-review encapsulates the latest findings (past 10 years) in the field of the deep eutectic solvents (DESs) application in the alkylation/arylation of different heterocyclic compounds. These solvents have been developed to fulfill the green chemistry concept demands and have been proven excellent for the application in various fields. This review describes their application in different types of alkylation,C-,N-,O- andS-alkylation.P-alkylation has not yet been published within this scope. Not only have the authors in this study proven that DESs could be successfully applied for this specific type of reaction, but they have also offered an excellent insight into the mechanisms of their action.

Pyrrolopyrimidine, A Multifaceted Scaffold in Cancer Targeted Therapy

Drug Research ◽  
2018 ◽  
Vol 68 (09) ◽  
pp. 485-498 ◽  
Author(s):  
Mai Adel ◽  
Rabah Serya ◽  
Deena Lasheen ◽  
Khaled Abouzid
Keyword(s):  
Clinical Trials ◽  
Heterocyclic Compounds ◽  
Kinase Inhibitors ◽  
Recent Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
The Us ◽  
Different Types ◽  
Us Fda ◽  
Cancer Targeted Therapy

AbstractPyrrolopyrimidine derivatives represent a class of biologically active heterocyclic compounds which can serve as promising scaffolds that display remarkable biological activities, such as anti-inflammatory, antimicrobial, antiviral and anticancer. In the last few years, several pyrrolopyrimidine derivatives have been approved by the US FDA and in other countries for the treatment of different diseases or are currently in phase I/II clinical trials. Due to their inimitable antioxidant and anti-tumor properties, researchers were inspired to develop novel derivatives for the treatment of different types of cancer. The present review summarizes recent literature up to 2017 on the most recent development in the medicinal chemistry of pyrrolopyrimidine derivatives and their potential as anticancer therapeutics, especially compounds acting as kinase inhibitors.

Recent Progress in the Synthesis of Pyrroles

2020 ◽  
Vol 24 (6) ◽  
pp. 622-657
Author(s):  
Duc Dau Xuan
Keyword(s):  
Biological Activity ◽  
Organic Semiconductors ◽  
Broad Spectrum ◽  
Heterocyclic Compounds ◽  
Recent Progress ◽  
Biological Activities ◽  
Antibacterial Activities ◽  
Synthetic Methods ◽  
Pyrrole Derivatives ◽  
Wide Range

: Pyrrole derivatives are nitrogen-containing heterocyclic compounds and widely distributed in a large number of natural and non-natural compounds. These compounds possess a broad spectrum of biological activities such as anti-infammatory, antiviral, antitumor, antifungal, and antibacterial activities. Besides their biological activity, pyrrole derivatives have also been applied in various areas such as dyes, conducting polymers, organic semiconductors. : Due to such a wide range of applicability, access to this class of compounds has attracted intensive research interest. Various established synthetic methods such as Paal-Knorr, Huisgen, and Hantzsch have been modified and improved. In addition, numerous novel methods for pyrrole synthesis have been discovered. This review will focus on considerable studies on the synthesis of pyrroles, which date back from 2014.

Structure, Biological Activities and Metabolism of Flavonoid Glucuronides

2021 ◽  
Vol 21 ◽  
Author(s):  
Min Chen ◽  
Xueyang Ren ◽  
Siqi Sun ◽  
Xiuhuan Wang ◽  
Xiao Xu ◽  
...  
Keyword(s):  
Natural Product ◽  
Biological Activities ◽  
Cerebrovascular Diseases ◽  
Diverse Range ◽  
Chemical Structures ◽  
The Past ◽  
Naturally Occurring ◽  
Notable Effect ◽  
Natural Product Research ◽  
Glycoside Bond

Background: Flavonoid glucuronides are a kind of natural products which present a flavone linked directly with one or several glucuronides through O-glycoside bond. They had become of interest in natural product research in the past decades for their antioxidant, anti-inflammatory, and anti-bacteria activities. In particular, the compound breviscapine has a notable effect on cardio-cerebrovascular diseases. Several other compounds even have antitumor activity. Methods: Through searching the database and reading a large number of documents, we summarized the related findings of flavonoid glucuronides. Results: We summarized 211 naturally occurring flavonoid glucuronides in 119 references with their chemical structures, biological activities, and metabolism. A total of 220 references from 1953 to 2020 were cited in this paper according to literature databases such as CNKI, Weipu, Wanfang data, Elsevier, Springer, Wiley, NCBI, PubMed, EmBase, etc. Conclusion : Flavonoid glucuronides are a class of compounds with various chemical structures and a diverse range of biological activities. And they are thought to be potential candidates for drug discovery, but the specific study on their mechanisms is still limited until now. We hope this article can provide references for natural product researchers and draw more attention to flavonoid glucuronides’ biological activities and mechanisms.

scholarly journals Novel Strategies in C-H Oxidations for Natural Product Diversification—A Remote Functionalization Application Summary

2021 ◽  
Vol 9 ◽  
Author(s):  
Huang Junrong ◽  
Yang Min ◽  
Dai Chuan ◽  
Zhou Yajun ◽  
Fang Huilong ◽  
...  
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Biological Activities ◽  
Product Diversification ◽  
Synthesis Methods ◽  
Chemical Bonds ◽  
Direct Oxidation ◽  
Bond Functionalization ◽  
Structure Activity ◽  
Challenges And Opportunities

Selectively activating the distal inactive C-H bond for functionalization is one of the on-going challenge in organic synthetic chemistry. In recent years, benefiting from the development of selective synthesis methods, novel methodologies not only make it possible to break non-traditional chemical bonds and attain more diversity in inactive sites, but also provide more possibilities for the diversification of complex natural products. Direct C-H bond functionalization approaches make it feasible to explore structure-activity relationship (SAR), generate metabolites and derivatives, and prepare biological probes. Among them, direct oxidation of inert C-H bonds is one of the most common methods for natural product diversification. In this review, we focus on the application of remote functionalization of inert C-H bonds for natural products derivatization, including the establishment of oxidation methods, the regulation of reaction sites, and the biological activities of derivatives. We highlight the challenges and opportunities of remote functionalization of inert C-H bonds for natural product diversification through selected and representative examples. We try to show that inert C-H bond oxidation, properly regulated and optimized, can be a powerful and efficient strategy in both synthetic and medicinal chemistry.

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