Recent Developments on Synthesis of Indole Derivatives Through Green Approaches and Their Pharmaceutical Applications

2020 ◽  
Vol 24 (22) ◽  
pp. 2665-2693
Author(s):  
Dipayan Mondal ◽  
Pankaj Lal Kalar ◽  
Shivam Kori ◽  
Shovanlal Gayen ◽  
Kalpataru Das
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Pharmaceutical Chemistry ◽  
Indole Derivatives ◽  
Biological Studies ◽  
Recent Developments ◽  
Pharmaceutical Industries ◽  
Green Methodology ◽  
Conventional Methods ◽  
High Yields

Indole moiety is often found in different classes of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, antihypertensive, anti-migraine, anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects the last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.

Synthetic Routes for 1,4-disubstituted 1,2,3-triazoles: A Review

2019 ◽  
Vol 23 (8) ◽  
pp. 860-900 ◽  
Author(s):  
Chander P. Kaushik ◽  
Jyoti Sangwan ◽  
Raj Luxmi ◽  
Krishan Kumar ◽  
Ashima Pahwa
Keyword(s):  
Solid Phase ◽  
Click Reaction ◽  
Biological Activities ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Biological Targets ◽  
Synthetic Routes ◽  
High Yields

N-Heterocyclic compounds like 1,2,3-triazoles serve as a key scaffolds among organic compounds having diverse applications in the field of drug discovery, bioconjugation, material science, liquid crystals, pharmaceutical chemistry and solid phase organic synthesis. Various drugs containing 1,2,3-triazole ring which are commonly available in market includes Rufinamide, Cefatrizine, Tazobactam etc., Stability to acidic/basic hydrolysis along with significant dipole moment support triazole moiety for appreciable participation in hydrogen bonding and dipole-dipole interactions with biological targets. Huisgen 1,3-dipolar azide-alkyne cycloaddition culminate into a mixture of 1,4 and 1,5- disubstituted 1,2,3-triazoles. In 2001, Sharpless and Meldal came across with a copper(I) catalyzed regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles by cycloaddition between azides and terminal alkynes. This azide-alkyne cycloaddition has been labelled as a one of the important key click reaction. Click synthesis describes chemical reactions that are simple to perform, gives high selectivity, wide in scope, fast reaction rate and high yields. Click reactions are not single specific reaction, but serve as a pathway for construction of simple to complex molecules from a variety of starting materials. In the last few decades, 1,2,3-triazoles attracted attention of researchers all over the world because of their broad spectrum of biological activities. Keeping in view the biological importance of 1,2,3-triazole, in this review we focus on the various synthetic routes for the syntheisis of 1,4-disubstituted 1,2,3-triazoles. This review involves various synthetic protocols which involves copper and non-copper catalysts, different solvents as well as substrates. It will boost synthetic chemists to explore new pathway for the development of newer biologically active 1,2,3-triazoles.

Anticancer Active Heterocyclic Chalcones: Recent Developments

2020 ◽  
Vol 20 ◽  
Author(s):  
Prasad Dandawate ◽  
Khursheed Ahmed ◽  
Subhash Padhye ◽  
Aamir Ahmad ◽  
Bernhard Biersack
Keyword(s):  
Histone Deacetylases ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Antitumor Activities ◽  
Web Based ◽  
Chemical Structures ◽  
Recent Developments ◽  
Number Of Publications ◽  
Tubulin Polymerization Inhibitors ◽  
Dna Binding Properties

Background: Chalcones are structurally simple compounds that are easily accessible by synthetic methods. Heterocyclic chalcones have gained the interest among scientists due to their diverse biological activities. The anti-tumor activities of heterocyclic chalcones are especially remarkable and the growing number of publications dealing with this topic warrants an up-to-date compilation. Methods: Search for antitumor active heterocyclic chalcones was carried out using Pubmed and Scifinder as common web-based literature searching tools. Pertinent and current literature is covered from 2015/2016 to 2019. Chemical structures, biological activities and modes of action of anti-tumor active heterocyclic chalcones are summarized. Results: Simply prepared chalcones have emerged over the last years with promising antitumor activities. Among them is a considerable number of tubulin polymerization inhibitors. But there are also new chalcones targeting special enzymes such as histone deacetylases or with DNA-binding properties. Conclusion: This review provides a summary of recent heterocyclic chalcone derivatives with distinct anti-tumor activities.

Recent Advancement of Pyrazole Scaffold Based Neuroprotective Agents: A Review

2021 ◽  
Vol 20 ◽  
Author(s):  
Subham Das ◽  
Saleem Akbar ◽  
Bahar Ahmed ◽  
Rikeshwar Prasad Dewangan ◽  
Mohammad Kashif Iqubal ◽  
...  
Keyword(s):  
Biological Activities ◽  
Neuroprotective Agents ◽  
Wide Range ◽  
Recent Developments ◽  
Ic50 Values ◽  
Structural Activity Relationship ◽  
Pharmaceutical Industries ◽  
Neurological Conditions ◽  
Nitrogen Containing Compounds

: As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact on chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various diseases, it has been identified as a biologically important heterocyclic scaffold. The treatment of neurological disorders has always been a difficult task. Therefore, identifying therapeutically effective molecules for neurological conditions remains an open challenge in biomedical research and development. For developing novel entities as neuroprotective agents, recently, pyrazole scaffold has attracted medicinal chemists worldwide. The major focus of research in this area is to discover novel molecules as neuroprotective agents with minimal adverse effects and better effectiveness in improving the neurological condition. This review mainly covers recent developments in the neuropharmacological role of pyrazole incorporated compounds, including their structural-activity relationship (SAR), which also further includes IC50 values (in mM as well as in μM), recent patents, and a brief history as neuroprotective agents.

Recent Advances in On-Water Multicomponent Synthesis of Coumarin Derivatives

2020 ◽  
Vol 24 (22) ◽  
pp. 2601-2611
Author(s):  
Komal Chandrakar ◽  
Jeevan Lal Patel ◽  
S. P. Mahapatra ◽  
Santhosh Penta
Keyword(s):  
Aqueous Medium ◽  
Biological Activities ◽  
Reaction Rates ◽  
Synthetic Methods ◽  
Sustainable Chemistry ◽  
Multicomponent Synthesis ◽  
Biologically Relevant ◽  
Naturally Occurring ◽  
Recent Developments ◽  
Made In

Coumarin-linked heterocycles represent privileged structural subunits and are welldistributed in naturally occurring compounds with immense biological activities. Multicomponent reactions (MCRs) are becoming a valuable tool for synthesizing structurally diverse molecular entities. On the other hand, the last year has seen a tremendous outburst in modifying chemical processes to make them sustainable for the betterment of our environment. The application of aqueous medium in organic synthesis is fulfilling some of the goals of ‘green and sustainable chemistry’ as it has some advantages over the traditional synthetic methods in terms of reaction rates, yields, purity of the products, product selectivity, etc. Hence, significant progress has been made in recent years. In the present review, we provide an overview of the recent developments of multicomponent synthesis of biologically relevant coumarin linked and fused heterocyclic compounds carried out from 2015 till today in an aqueous medium.

Recent Developments in the Synthesis and Antimicrobial Activity of Indole and its Derivatives

2019 ◽  
Vol 16 (1) ◽  
pp. 17-37 ◽  
Author(s):  
Jaskirat Kaur ◽  
Divya Utreja ◽  
Ekta ◽  
Nisha Jain ◽  
Shivali Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Microbial Activity ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Antimicrobial Properties ◽  
Biological Properties ◽  
Indole Derivatives ◽  
Antimicrobial Drugs ◽  
Wide Range ◽  
Recent Developments

Background:Heterocyclic compounds containing nitrogen have been known to possess a very important role in the field of medicinal chemistry. Indole and its derivatives displayed a wide range of biological properties such as anti-inflammatory, analgesic, anti-microbial, anti-convulsant, antidepressant, anti-diabetic, antihelmintic and anti-allergic activities etc. The diverse biological activities exhibited by compounds containing indole moiety has provided the impetus to explore its anti-microbial activity in order to save the valuable life of patients. </P><P> Objective: The review focuses on the advances in the synthesis of indole derivatives and antimicrobial properties exhibited by them.Conclusion:A great deal of work has been done in order to synthesize indole derivatives and to evaluate antimicrobial potential, as indicated by the review. The information provided in this article may be helpful for the researchers for the development of efficient antimicrobial drugs.

scholarly journals Chemical Characteristics, Synthetic Methods, and Biological Potential of Quinazoline and Quinazolinone Derivatives

2014 ◽  
Vol 2014 ◽  
pp. 1-27 ◽  
Author(s):  
Mohammad Asif
Keyword(s):  
Broad Spectrum ◽  
Biological Activities ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Pharmaceutical Chemistry ◽  
Chemical Characteristics ◽  
Biological Potential ◽  
Antileishmanial Activities ◽  
Quinazolinone Derivatives ◽  
Anti Hiv

The heterocyclic fused rings quinazoline and quinazolinone have drawn a huge consideration owing to their expanded applications in the field of pharmaceutical chemistry. Quinazoline and quinazolinone are reported for their diversified biological activities and compounds with different substitutions bring together to knowledge of a target with understanding of the molecule types that might interact with the target receptors. Quinazolines and quinazolinones are considered as an important chemical for the synthesis of various physiological significance and pharmacological utilized molecules. Quinazolines and quinazolinone are a large class of biologically active compounds that exhibited broad spectrum of biological activities such as anti-HIV, anticancer, antifungal, antibacterial, antimutagenic, anticoccidial, anticonvulsant, anti-inflammatory, antidepressant, antimalarial, antioxidant, antileukemic, and antileishmanial activities and other activities. Being considered as advantaged scaffold, the alteration is made with different substituent.

scholarly journals A Review on Silver Nanoparticles: Classification, Various Methods of Synthesis, and Their Potential Roles in Biomedical Applications and Water Treatment

Water ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 2216
Author(s):  
Muhammad Zahoor ◽  
Nausheen Nazir ◽  
Muhammad Iftikhar ◽  
Sumaira Naz ◽  
Ivar Zekker ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Water Treatment ◽  
Biomedical Applications ◽  
Biological Activities ◽  
Chemical Reduction ◽  
Synthetic Methods ◽  
Environment Friendly ◽  
Dispersing Agent ◽  
Methods Of Synthesis ◽  
Recent Developments

Recent developments in nanoscience have appreciably modified how diseases are prevented, diagnosed, and treated. Metal nanoparticles, specifically silver nanoparticles (AgNPs), are widely used in bioscience. From time to time, various synthetic methods for the synthesis of AgNPs are reported, i.e., physical, chemical, and photochemical ones. However, among these, most are expensive and not eco-friendly. The physicochemical parameters such as temperature, use of a dispersing agent, surfactant, and others greatly influence the quality and quantity of the synthesized NPs and ultimately affect the material’s properties. Scientists worldwide are trying to synthesize NPs and are devising methods that are easy to apply, eco-friendly, and economical. Among such strategies is the biogenic method, where plants are used as the source of reducing and capping agents. In this review, we intend to debate different strategies of AgNP synthesis. Although, different preparation strategies are in use to synthesize AgNPs such as electron irradiation, optical device ablation, chemical reduction, organic procedures, and photochemical methods. However, biogenic processes are preferably used, as they are environment-friendly and economical. The review covers a comprehensive discussion on the biological activities of AgNPs, such as antimicrobial, anticancer anti-inflammatory, and anti-angiogenic potentials of AgNPs. The use of AgNPs in water treatment and disinfection has also been discussed in detail.

scholarly journals RECENT DEVELOPMENTS AND MULTIPLE BIOLOGICAL ACTIVITIES AVAILABLE WITH 1, 8-NAPHTHYRIDINE DERIVATIVES: A REVIEW

2019 ◽  
pp. 17-37
Author(s):  
Vinod Kumar Gurjar ◽  
Dilipkumar Pal
Keyword(s):  
Biological Activities ◽  
Neurological Diseases ◽  
Growth Factor Receptor ◽  
Pharmaceutical Chemistry ◽  
Pharmacological Activities ◽  
Egfr Inhibition ◽  
Wide Range ◽  
Versatile Tool ◽  
Recent Developments ◽  
Derivatives Of

Within the wide range of nitrogen-containing heterocyclic compounds, the derivatives of 1,8-naphthyridine (NPTR) have gained a rising interest due to their reported versatile biological activities. The derivatives of NPTR scaffold are found to invite special interest from researchers nowadays on the significance of their manifestations of multiple attractive pharmacological activities which establish them as an effective and versatile tool in pharmaceutical chemistry and drug discovery. The diverse biological activities mainly include anti-inflammatory, antimicrobial, antiviral, anticancer, antihypertensive and analgesic activities. Novel NPTR scaffold has emerged its potency to treat neurological diseases like depression and Alzheimer's disease. Further these agents possess different inhibitory activities, such as anti-HIV, anti-osteoporotic, αvβ3 antagonism, antimalarial, platelet aggregation, anti-oxidant, anti-allergic, gastric antisecretory, anticonvulsant, epidermal growth factor receptor (EGFR) inhibition, protein kinase inhibition, ionotropic properties, β3 antagonism, phosphodiesterase 4 (PDE 4) inhibitions, adenosine receptor agonistic activity, adrenoceptors antagonism and DNA stabilizing activity, etc. In this review, we highlight the updates of different 1,8-naphthyridine derivatives and explain the key data available in the context of various biological activities of NPTR derivatives available from the literature. This may direct opportunity in researches in the synthesis of novel medicinal agents and the development of new heterocycles for modification of existing biological actions as well as evaluation of other possible pharmacological activities.

Recent Developments in the Synthesis of Cinnoline Derivatives

2019 ◽  
Vol 16 (6) ◽  
pp. 578-588 ◽  
Author(s):  
Kamal Usef Sadek ◽  
Ramadan Ahmed Mekheimer ◽  
Mohamed Abd-Elmonem
Keyword(s):  
Reaction Mechanisms ◽  
Biological Activities ◽  
Bond Formation ◽  
Pharmaceutical Chemistry ◽  
Recent Developments ◽  
Synthetic Routes ◽  
Anti Inflammatory ◽  
Arenediazonium Salts ◽  
Metal Catalyzed ◽  
Bond Formation Reactions

Crinnolines can serve as unique and versatile class of heterocycles especially in fields related to synthetic and pharmaceutical chemistry owing to their potent biological activities. They possess diversity of pharmaceutical activities as anticancer, antibacterial, anti-inflammatory, anti-allergic as well as anti-hypertensive activities. Since the first synthesis of cinnoline by Richter (1883) numerous protocols for their synthesis have been developed utilizing arenediazonium salts, aryl hydrazines and arylhydhydrazones precursors. Recently metal catalyzed C-C and C-N bond formation reactions have emerged as efficient tools for synthesis of cinnoline derivatives. This review aims to focus on the recent synthetic routes used for the synthesis of cinnoline derivatives. An effort has been carried out to provide an overview of practical methods for preparing cinnolines. Furthermore the reaction mechanisms have been described in brief.

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.

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