Quinoxaline as Ubiquitous Structural Fragment: An update on the recent development of its Green Synthetic Approaches

2021 ◽  
Vol 25 ◽  
Author(s):  
Ashish Patel ◽  
Drashti Shah ◽  
Naiya Patel ◽  
Khushbu Patel ◽  
Nidhi Soni ◽  
...  
Keyword(s):  
Biological Activities ◽  
Ultrasound Irradiation ◽  
Daily Basis ◽  
Structural Fragment ◽  
Current State ◽  
Short Period ◽  
Wide Range ◽  
Quinoxaline Derivatives ◽  
Benign Solvents ◽  
Synthetic Approaches

: Quinoxaline is a versatile heterocyclic moiety that possesses a wide range of biological activities. Therefore, many researchers have been performing the synthesis of quinoxaline derivatives on a daily basis. In addition, high demands for their synthesis often result in an increased generation of different waste chemicals. However, to minimize the utilization and generation of toxic organic substances, the present review focuses on the various green synthetic approaches for the synthesis of quinoxaline and its derivatives. Moreover, due to the quick manufacturing of novel medications using a quinoxaline scaffold, multiple study reports are published in a short period of time. Therefore, to fully comprehend the current state of the quinoxaline scaffold in medicinal chemistry, it is necessary to combine recent findings with previous understanding. Besides, compared to conventional methods, these green methods minimize the use and generation of harmful chemicals and improve reaction efficiency in terms of product yields, purity, energy consumption, and post-synthetic procedures. Therefore, in this review, we have attempted to shed light on various green synthetic strategies leading to the synthesis of quinoxaline scaffold and its derivatives, such as ultrasound irradiation, microwave irradiation, grindstone technique, environmentally benign solvents/catalysts based, and reactant immobilized on a solid support, etc.

scholarly journals Synthesis of 3-Amino-4-Substituted Monocyclic ß-Lactams—Important Structural Motifs in Medicinal Chemistry

2021 ◽  
Vol 23 (1) ◽  
pp. 360
Author(s):  
Katarina Grabrijan ◽  
Nika Strašek ◽  
Stanislav Gobec
Keyword(s):  
Important Determinant ◽  
Biological Activities ◽  
Cholesterol Absorption ◽  
Pharmacological Activities ◽  
Cerium Ammonium Nitrate ◽  
Wide Range ◽  
Cerium Ammonium ◽  
Ring Nitrogen ◽  
Inhibitory Activities ◽  
Synthetic Approaches

Monocyclic ß-lactams (azetidin-2-ones) exhibit a wide range of biological activities, the most important of which are antibacterial, anticancer, and cholesterol absorption inhibitory activities. The synthesis of decorated monocyclic ß-lactams is challenging because their ring is highly constrained and consequently reactive, which is also an important determinant of their biological activity. We present the optimized synthesis of orthogonally protected 3-amino-4-substituted monocyclic ß-lactams. Among several possible synthetic approaches, Staudinger cycloaddition proved to be the most promising method for initial ring formation, yielding monocyclic ß-lactams with different substituents at the C-4 position, a phthalimido-protected 3-amino group, and a (dimethoxy)benzyl protected ring nitrogen. Challenging deprotection methods were then investigated. Oxidative cleavage with cerium ammonium nitrate and ammonia-free Birch reduction was found to be most effective for selective removal of ring nitrogen protection. Hydrazine hydrate was used for deprotection of the phthalimido group, and the procedure had to be modified by the addition of HCl in the case of aromatic substituents at the C-4 position. The presented methods and the synthesized 3-amino-4-substituted monocyclic ß-lactam derivatives are an important step toward new ß-lactams with potential pharmacological activities.

Green Chemistry Approaches to the Synthesis of Coumarin Derivatives

2020 ◽  
Vol 24 (1) ◽  
pp. 4-43 ◽  
Author(s):  
Maja Molnar ◽  
Melita Lončarić ◽  
Marija Kovač
Keyword(s):  
Energy Consumption ◽  
Green Chemistry ◽  
Biological Activities ◽  
Daily Basis ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Specific Class ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Coumarin Synthesis

This review is a compilation of the green synthetic methods used in the synthesis of coumarin derivatives. Coumarins are a class of compounds with a pronounced wide range of biological activities, which have found their application in medicine, pharmacology, cosmetics and food industry. Their biological activity and potential application are highly dependent on their structure. Therefore, many researchers have been performing the synthesis of coumarin derivatives on a daily basis. High demands for their synthesis often result in an increased generation of different waste chemicals. In order to minimize the utilization and generation of toxic organic substances, green synthetic methods are applied in this manner. These methods are getting more attention in the last few decades. Green chemistry methods cover a wide range of methods, including the application of ultrasound and microwaves, ionic liquids and deep eutectic solvents, solvent-free synthesis, mechanosynthesis and multicomponent reactions. All typical condensation reactions for coumarin synthesis like Knoevenagel, Perkin, Kostanecki-Robinson, Pechmann and Reformansky reactions, have been successfully performed using these green synthetic methods. According to the authors mentioned in this review, not only these methods reduce the utilization and generation of toxic chemicals, but they can also enhance the reaction performance in terms of product yields, purity, energy consumption and post-synthetic procedures when compared to the conventional methods. Due to the significance of coumarins as biologically active systems and the recent demands of reducing toxic solvents, catalysts and energy consumption, this review provides a first full literature overview on the application of green synthetic methods in the coumarin synthesis. It covers a literature search over the period from 1995-2019. The importance of this work is its comprehensive literature survey on a specific class of heterocyclic compounds, and those researchers working on the coumarin synthesis can find very useful information on the green synthetic approaches to their synthesis. There are some reviews on the coumarin synthesis, but most of them cover only specific reactions on coumarin synthesis and none of them the whole range of green chemistry methods.

(Hetero)Aryloxyaminopropanols with N-Phenylpiperazine Structural Fragment – Review of Cardiovascular Activity

2020 ◽  
Vol 20 (17) ◽  
pp. 1719-1731
Author(s):  
Pavlina Marvanova ◽  
Tereza Padrtova ◽  
Petr Mokry
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Biological Activities ◽  
Cardiovascular Effects ◽  
Structural Fragment ◽  
Cardiovascular Activity ◽  
Phosphodiesterase Inhibition ◽  
Cardiovascular Agents ◽  
Wide Range ◽  
The Central Nervous System

Aryloxyphenylpiperazinylpropanols are a group of compounds exhibiting a wide range of biological activities, affecting the central nervous system and many cardiovascular mechanisms among them. As cardiovascular agents, aryloxyphenylpiperazinylpropanols work as antihypertensives, antiarrhythmics, cardiotonics or antiaggregants. The mechanism of action is almost always an α1-adrenolytic or combined α1- and β-adrenolytic effect, but sometimes other mechanisms (e.g., Ca2+ antagonism or phosphodiesterase inhibition) antagonism or phosphodiesterase inhibition) can positively participate. In some cases, compounds with a small modification of the connecting chain also exhibit the desired cardiovascular effects. Several studies dealt with chirality of aryloxyphenylpiperazinylpropanols and determined the differences between the particular activities of racemic and enantiomeric compounds.

Halogenated Flavones and Isoflavones: A State-of-Art on their Synthesis

2020 ◽  
Vol 17 (6) ◽  
pp. 415-425
Author(s):  
Ricardo Santos ◽  
Diana Pinto ◽  
Clara Magalhães ◽  
Artur Silva
Keyword(s):  
Biological Activities ◽  
New Drugs ◽  
Reaction Conditions ◽  
Balanced Diet ◽  
Wide Range ◽  
The Everyday ◽  
Synthetic Routes ◽  
Scopus Database ◽  
Reported Data ◽  
Synthetic Approaches

Background: Flavonoid is a family of compounds present in the everyday consumption plants and fruits, contributing to a balanced diet and beneficial health effects. Being a scaffold for new drugs and presenting a wide range of applicability in the treatment of illnesses give them also an impact in medicine. Among the several types of flavonoids, flavone and isoflavone derivatives can be highlighted due to their prevalence in nature and biological activities already established. The standard synthetic route to obtain both halogenated flavones and isoflavones is through the use of already halogenated starting materials. Halogenation of the flavone and isoflavone core is less common because it is more complicated and involves some selectivity issues. Objective: Considering the importance of these flavonoids, we aim to present the main and more recent synthetic approaches towards their halogenation. Methods: The most prominent methodologies for the synthesis of halogenated flavones and isoflavones were reviewed. A careful survey of the reported data, using mainly the Scopus database and halogenation, flavones and isoflavones as keywords, was conducted. Results: Herein, a review is provided on the latest and more efficient halogenation protocols of flavones and isoflavones. Selective halogenation and the greener methodologies, including enzymatic and microbial halogenations, were reported. Nevertheless, some interesting protocols that allowed the synthesis of halogenated flavone and isoflavone derivatives in specific positions using halogenated reagents are also summarized. Conclusion: Halogenated flavones and isoflavones have risen as noticeable structures; however, most of the time, the synthetic procedures involve toxic reagents and harsh reaction conditions. Therefore, the development of new synthetic routes with low environmental impact is desirable.

Benzimidazole as Ubiquitous Structural Fragment : An Update on Development of its Green Synthetic Approaches

2020 ◽  
Vol 17 ◽  
Author(s):  
Ashish Patel ◽  
Drashti Shah ◽  
Naiya Patel ◽  
Khushbu Patel ◽  
Nidhi Soni ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Ultrasound Irradiation ◽  
Heating Time ◽  
Biologically Active ◽  
New Drugs ◽  
Current Status ◽  
Benzimidazole Derivatives ◽  
Structural Fragment ◽  
Short Period

Abstract: The benzimidazole and its derivatives are privileged heterocyclic motif and important building block for the development of the biologically active compound. However, several research reports are produced in a short period of time due to the rapid production of new drugs having a benzimidazole nucleus. In order to understand the current status of the benzimidazole nucleus in medicinal chemistry science, it is therefore important to combine the latest knowledge with earlier information. Hence, synthetic organic chemists concentrated on inventing an effective green methodology for synthesizing benzimidazole derivatives. In addition to this, non-degradable chemical compounds cause the ecosystem to become fragile, damage or irritation as contaminants and pose a danger to the environment. However, conventional methods of synthesis need longer heating time, complicated and tedious apparatus set up which result in high cost and pollution in contrast to greener methods which are inexpensive. In the present review, therefore, we have attempted to shed light on various synthetic strategies leading to the synthesis of different benzimidazole derivatives through the direct condensation reaction between o-phenylenediamine and aromatic aldehydes using green chemistry approaches such as mechanochemistry, ultrasound irradiation, microwave irradiation, environmentally benign solvents/catalysts, reactant immobilized on a solid support and blue light irradiation.

scholarly journals An Overview of Coumarin as a Versatile and Readily Accessible Scaffold with Broad-Ranging Biological Activities

2020 ◽  
Vol 21 (13) ◽  
pp. 4618 ◽  
Author(s):  
Francesca Annunziata ◽  
Cecilia Pinna ◽  
Sabrina Dallavalle ◽  
Lucia Tamborini ◽  
Andrea Pinto
Keyword(s):  
Scientific Community ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Natural Compounds ◽  
Natural Sources ◽  
Wide Range ◽  
Living Organisms ◽  
Privileged Structures ◽  
Synthetic Approaches ◽  
Critical Overview

Privileged structures have been widely used as an effective template for the research and discovery of high value chemicals. Coumarin is a simple scaffold widespread in Nature and it can be found in a considerable number of plants as well as in some fungi and bacteria. In the last years, these natural compounds have been gaining an increasing attention from the scientific community for their wide range of biological activities, mainly due to their ability to interact with diverse enzymes and receptors in living organisms. In addition, coumarin nucleus has proved to be easily synthetized and decorated, giving the possibility of designing new coumarin-based compounds and investigating their potential in the treatment of various diseases. The versatility of coumarin scaffold finds applications not only in medicinal chemistry but also in the agrochemical field as well as in the cosmetic and fragrances industry. This review is intended to be a critical overview on coumarins, comprehensive of natural sources, metabolites, biological evaluations and synthetic approaches.

Synthetic Investigations On Medicinally Important Quinoxaline Scaffold: A Mini Review.

2020 ◽  
Vol 17 ◽  
Author(s):  
Nitin Kumar ◽  
Niranjan Kaushik ◽  
Shiv Kumar ◽  
Vikas Sharma
Keyword(s):  
Biological Activities ◽  
Review Article ◽  
Synthetic Methods ◽  
Present Review ◽  
The Past ◽  
Quinoxaline Derivatives ◽  
Almost All ◽  
Synthetic Approaches ◽  
Heterocyclic Moiety

: Quinoxaline is a versatile heterocyclic moiety that posses almost all types of biological activities. Present work is a sincere attempt to review synthetic investigations of quinoxaline. A wide plethora of literature is available possessing different synthetic methods utilized for the synthesis of quinoxaline based scaffolds. The present review focuses on the various synthetic approaches of quinoxaline derivatives, which includes a summary of the advancement made over the past years in the synthesis of quinoxaline nucleus and its derivatives. Some of these methods are mentioned in the review article associated with industrial applicability.

Anodyne activities of New Tetrazole derivatives from Triazine

2020 ◽  
Vol 11 (3) ◽  
pp. 3377-3383
Author(s):  
Arulmozhi R ◽  
Abirami N ◽  
Helen P Kavitha ◽  
Arulmurugan S ◽  
Vinoth Kumar J
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Pharmaceutical Chemistry ◽  
Tail Flick ◽  
Structural Fragment ◽  
Hot Plate ◽  
Standard Drug ◽  
New Class ◽  
Novel Drugs ◽  
Tetrazole Derivatives

The creation of novel drugs containing a tetrazole ring as a structural fragment has contributed considerably to the outstanding achievements of the pharmaceutical chemistry in the last decade. Tetrazoles are the heterocyclic compounds having diverse biological activities such as analgesic, antiinflammation, antimicrobial, anticancer, antidiabetic, etc., and an impending source in biosciences. In this paper, the authors describe the synthesis of novel tetrazoles from N, N-( 6-Phenyl-1,3,5-triazine-2,4-diyl) dibenzamide (PTDDB) and 2-phenyl-4, 6-di(2H-tetrazole-2-yl)-1,3,5-triazine(5a-i) were prepared per the proposed scheme. A new class of tetrazole heterocycles were synthesised and characterised. I n vivo analysis was carried out on the analgesic property of synthesised tetrazole derivatives (5a, 5b, 5c). Characterisation studies such as IR, 1H NMR, 13C NMR, Mass and elemental analysis were performed for the synthesised tetrazole derivatives. Some of the tetrazole derivatives 5a, 5b, and 5c were tested for anodyne activity using morphine as the standard drug. The data reveals that all the three compounds 5a, 5b and 5c taken for the study show analgesic activity by hot plate method and tail flick methods. Among tested compounds, compound 5c is found to have potent analgesic (anodyne) activity. The results of the study indicate that the sample taken for the study show fairly good business using morphine as the standard drug.

Young Scholars Conference “Slavic World: Commonality and Diversity”. 21–22 May 2019. Session “Linguistics”

2019 ◽  
Vol 14 (1-2) ◽  
pp. 295-297
Author(s):  
Sergej A. Borisov
Keyword(s):  
Czech Republic ◽  
Middle Ages ◽  
The Czech Republic ◽  
International Context ◽  
Slavic Languages ◽  
Russian Academy Of Sciences ◽  
Current State ◽  
Wide Range ◽  
History Of ◽  
Academy Of Sciences

For more than twenty years, the Institute of Slavic Studies of the Russian Academy of Sciences celebrates the Day of Slavic Writing and Culture with a traditional scholarly conference.”. Since 2014, it has been held in the young scholars’ format. In 2019, participants from Moscow, St. Petersburg, Kazan, Togliatti, Tyumen, Yekaterinburg, and Rostov-on-Don, as well as Slovakia, the Czech Republic, Hungary, and Romania continued this tradition. A wide range of problems related to the history of the Slavic peoples from the Middle Ages to the present time in the national, regional and international context were discussed again. Participants talked about the typology of Slavic languages and dialects, linguo-geography, socio- and ethnolinguistics, analyzed formation, development, current state, and prospects of Slavic literatures, etc.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Sign in / Sign up

Export Citation Format

Share Document