Green Chemistry Synthesis Methods of Oxazine and Thiazine Derivatives as Promising Scaffolds in Medicinal Chemistry: A Mini-Review

Author(s):  
Mohammad Asif ◽  
Mohammad Imran

: Green synthesis of oxazine and thiazine derivatives have concerned a great impact of concern of medicinal researchers and provided a lead molecule for the design and development of various potential bioactive molecules. This review associated additional green synthetic information and it would extend a great deal of help to researchers in synthesizing the most productive, economical, and clinically important thiazine and oxazine derivatives which will be expected to show potent pharmacological activities. This has led to the discovery of various compounds that have diverse types of interesting biological activities. Propose of this article is to study the various synthetic methods of oxazine and thiazine derivatives by green chemistry methods and their biological activities. We expect that this article will be interesting for researchers concerned with oxazine and thiazine compounds.

2021 ◽  
Vol 7 (1) ◽  
pp. 18-27
Author(s):  
Mohammad Asif

Purpose: The chemistry society has activated to expand new chemistry that is less destructive to the environment and human health. This approach has extensive interest and designated as green chemistry, environmentally friendly chemistry, clean chemistry, and atom economy. Methodology: There is advancement toward involved chemistry with the facts and do not prevent the properties of the target compound or the efficacy of particular solvents or reagents. The use of chemistry in a way that maximizes benefits while reducing adverse effects has come to be green chemistry. Main findings: Reduce the use and formation of harmful products or by-products. Presently maximum pollution to the environment is caused by some chemical industries. So, need to design and develop synthetic methods in such a way that the waste products are lowest and have no effect on the environment and their handy disposal. Applications of the work: Green chemistry plays a vital role in pharmaceuticals for developing new drugs which are less toxic, more effective with low side effects. The novelty of the work: The industries performing manufacturing using green synthesis methods to carrying out their productions have positive impacts on environmental sustainability. This review is looking ahead at longer-term challenges and prospects in research, industrial applications, and education.


2020 ◽  
Vol 17 (3) ◽  
pp. 323-350
Author(s):  
Mahesh Bhat ◽  
Shiddappa Lagamappa Belagali

:Benzothiazole (1, 3-benzothiazole) is one of the heterocyclic compounds, which is a weak base having varied biological activities. The unique methine center present in the thiazole ring makes benzothiazole as the most important heterocyclic compound. It is a common and integral structure of many natural and synthetic bioactive molecules. Benzothiazole derivatives show a variety of activities, with less toxic effects and their derivatives showed enhanced activities, which has proven Benzothiazole scaffold as one of the important moieties in medicinal chemistry. Benzothiazole ring containing compounds possess various pharmacological activities such as anti-viral, anti-microbial, antiallergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer, which makes benzothiazole a rapidly developing and interesting compound in the medicinal chemistry. This review briefly explains the importance, common methods of synthesis of the benzothiazole scaffold and also explains the popular benzothiazole molecules which have applications in various fields of chemistry. A review has been carried out based on various pharmacological activities containing benzothiazole moieties and rationalize the activities based on the structural variations. Literature on benzothiazole derivatives reveals that substitution on the C-2 carbon atom and C-6 are the reasons for a variety of biological activities.


Author(s):  
Anikate Sood ◽  
Shweta Agarwal

Nanotechnology is the most sought field in biomedical research. Metallic nanoparticles have wide applications in the medical field and have gained the attention of various researchers for advanced research for their application in pharmaceutical field. A variety of metallic nanoparticles like gold, silver, platinum, palladium, copper and zinc have been developed so far. There are different methods to synthesize metallic nanoparticles like chemical, physical, and green synthesis methods. Chemical and physical approaches suffer from certain drawbacks whereas green synthesis is emerging as a nontoxic and eco-friendly approach in production of metallic nanoparticles. Green synthesis is further divided into different approaches like synthesis via bacteria, fungi, algae, and plants. These approaches have their own advantages and disadvantages. In this article, we have described various metallic nanoparticles, different modes of green synthesis and brief description about different metabolites present in plant that act as reducing agents in green synthesis of metallic nanoparticles. 


2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi

Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and pharmacological activities of pyrimidine nucleus.


2019 ◽  
Vol 15 ◽  
pp. 388-400
Author(s):  
Pedro N Batalha ◽  
Luana da S M Forezi ◽  
Maria Clara R Freitas ◽  
Nathalia M de C Tolentino ◽  
Ednilsom Orestes ◽  
...  

4-Oxoquinolines are a class of organic substances of great importance in medicinal chemistry, due to their biological and synthetic versatility. N-1-Alkylated-4-oxoquinoline derivatives have been associated with different pharmacological activities such as antibacterial and antiviral. The presence of a carboxamide unit connected to carbon C-3 of the 4-oxoquinoline core has been associated with various biological activities. Experimentally, the N-ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide occurs at the nitrogen of the oxoquinoline group, in a regiosselective way. In this work, we employed DFT methods to investigate the regiosselective ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide, evaluating its acid/base behavior and possible reaction paths.


Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 42 ◽  
Author(s):  
Alina Secrieru ◽  
Paul Michael O’Neill ◽  
Maria Lurdes Santos Cristiano

Pyrazoles are known as versatile scaffolds in organic synthesis and medicinal chemistry, often used as starting materials for the preparation of more complex heterocyclic systems with relevance in the pharmaceutical field. Pyrazoles are also interesting compounds from a structural viewpoint, mainly because they exhibit tautomerism. This phenomenon may influence their reactivity, with possible impact on the synthetic strategies where pyrazoles take part, as well as on the biological activities of targets bearing a pyrazole moiety, since a change in structure translates into changes in properties. Investigations of the structure of pyrazoles that unravel the tautomeric and conformational preferences are therefore of upmost relevance. 3(5)-Aminopyrazoles are largely explored as precursors in the synthesis of condensed heterocyclic systems, namely pyrazolo[1,5-a]pyrimidines. However, the information available in the literature concerning the structure and chemistry of 3(5)-aminopyrazoles is scarce and disperse. We provide a revision of data on the present subject, based on investigations using theoretical and experimental methods, together with the applications of the compounds in synthesis. It is expected that the combined information will contribute to a deeper understanding of structure/reactivity relationships in this class of heterocycles, with a positive impact in the design of synthetic methods, where they take part.


2020 ◽  
Vol 24 (1) ◽  
pp. 4-43 ◽  
Author(s):  
Maja Molnar ◽  
Melita Lončarić ◽  
Marija Kovač

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.


2018 ◽  
Vol 18 (17) ◽  
pp. 1428-1453 ◽  
Author(s):  
Luana da S.M. Forezi ◽  
Mariana F.C. Cardoso ◽  
Daniel T.G. Gonzaga ◽  
Fernando de C. da Silva ◽  
Vitor F. Ferreira

Heterocyclic rings having nitrogen atoms are the molecular fragments most used in drug design by using the tools of medicinal chemistry. The 1,2,4-triazole rings are part of an extensive family of drugs that are in use in the pharmaceutical market. More recently, 1,2,3-triazole rings have begun to arouse the great interest of scientists and therefore, many researches have been developed seeking the synthesis of new substances and their possible biological activities. A number of articles have been published by us and others highlighting the synthetic and biological aspects of 1,2,3-triazoles. The growth of new substances of this class was largely due to the simple and selective synthetic method of 1,2,3- triazole ring developed by Sharpless et al. However, some 1,2,3-triazole cannot be synthesized by this method. This review focuses on other synthetic methods that give access to other variations around the 1,2,3-triazole core. The systematic arrangement in this review explores the possibility of providing practical guidance to alternatives of this heterocycle. It has been divided into sections according to the types of starting materials and reactions.


2020 ◽  
Vol 17 (5) ◽  
pp. 574-584 ◽  
Author(s):  
Pratiksha N. Chopra ◽  
Jagdish K. Sahu

In the field of heterocyclic medicinal chemistry, especially five-membered ring structures containing a nitrogen atom, imidazole core is an imperative aromatic heterocycle which is usually present in naturally occurring products and synthetic bioactive molecules. The occurrence of imidazole moiety in therapeutic compounds may be beneficial in terms of improving water-soluble properties due to its two nitrogen atoms which leads to the creation of hydrogen bonds. The imidazole nucleus has also been recognized as an important isostere of triazole, pyrazole, thiazole, tetrazole, oxazole, amide etc. for the purpose of designing and development of various biologically active molecules. Moreover, imidazole core as an attractive binding site could interact with diverse cations and anions as well as biomolecules through different reactions in the human biological system thus displaying extensive biological activities. This effort thoroughly provides a wide-ranging assessment in current drug discovery and developments of imidazolebased analogues in the entire series of synthetic medicinal chemistry as antibacterial and antifungal, anticancer, anti-tubercular, analgesic and anti-inflammatory, anti-neuropathic, antihypertensive, anti-allergic, anti-parasitic, antiviral, antidepressant, anti-obesity and so on, altogether with their prospective approaches in diagnostic and pathological field. It is expected that the present review will be supportive on behalf of new opinions in the search for rational strategies of more efficacious and less toxic medicinal agents and drugs containing imidazole core.


Author(s):  
Lucas F. E. Moor ◽  
Thatyana R. A. Vasconcelos ◽  
Raisa da R. Reis ◽  
Ligia S. S. Pinto ◽  
Thamires M. da Costa

: Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. In fact, the quinoline nucleus is found in the structure of many drugs and in rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019) focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti-Leishmania and anti-Alzheimer’s disease.


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