1,8-Naphthyridine derivatives: A privileged scaffold for versatile biological activities

2020 ◽  
Vol 20 ◽  
Author(s):  
Madhwi Ojha ◽  
Divya Yadav ◽  
Avinash Kumar ◽  
Suman Dasgupta ◽  
Rakesh Yadav
Keyword(s):  
Heterocyclic Compounds ◽  
Receptor Agonist ◽  
Biological Activities ◽  
Biological Properties ◽  
Present Review ◽  
Anti Psychotic ◽  
Cb2 Receptor ◽  
Research Groups ◽  
Anti Cancer ◽  
Privileged Scaffold

: 1, 8- Naphthyridine nucleus belongs to significant nitrogen-containing heterocyclic compounds which have garnered the interest of researchers due to its versatile biological activities. It is known to be used as an antimicrobial, anti-psychotic, anti-depressant, anti-convulsant, anti-Alzheimer’s, anti-cancer, analgesic, anti-inflammatory, antioxidant, anti-viral, anti-hypertensive, anti-malarial, pesticides, anti-platelets, and CB2 receptor agonist, etc. The present review highlights the framework of biological properties of synthesized 1, 8-naphthyridine derivatives developed by various research groups across the globe.

scholarly journals 1,2,3-Triazoles: Lead Molecules For Promising Drugs: A Review

2021 ◽  
Vol 33 (12) ◽  
pp. 2896-2918
Author(s):  
Rakesh Singh ◽  
Harpreet Kaur ◽  
Pankaj Gupta
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Parent Nucleus ◽  
Biological Properties ◽  
Biologically Active ◽  
Hiv Protease ◽  
Present Review ◽  
Hiv Protease Inhibitors ◽  
Drug Molecules ◽  
Wide Range

A large number of heterocyclic compounds with five membered rings as the parent nucleus such as tetrazoles, imidazoles, triazoles, oxadiazoles, thiadiazoles, thiazoles, etc. have been studied extensively owing to their fascinating biological properties like anticancer, antifungal, antimicrobial, antitumor, anticonvulsant, antiviral, etc. 1,2,3-Triazoles are important class of five-membered biologically active heterocyclic compounds as they exhibit wide range of pharmacological activities. Triazoles are of two types viz. 1,2,3-triazole and 1,2,4-triazole. These compounds have drawn great attention from chemists and biologists since their discovery. In recent years, triazoles has emerged as an interesting field in drug design for many researchers due to their enormous pharmacological scope. The present review aims to sum up the medicinal significance of 1,2,3-triazoles as one of the most significant structures for the development of drug molecules like anticancer, antibacterial, HIV protease inhibitors, antifungal, anti-inflammatory (COX-1/COX-2 inhibitors), antiprotozoal, anticonvulsant, antioxidant and others, which are under clinical trials. Various benzyl and benzyl-halide functionalized 1,2,3-triazole derivatives like rufinamide, mubritinib (TAK-165) and suvorexant showing excellent biological activities have been used as medicine. In present review, more stress has been laid on the major developments in the therapeutic aspects of triazole pharmacophore for the last two decades.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

scholarly journals Antitumor Activities of Flavonoids and Their Biological Activities on Human Health: الفلافونويدات المضادة للأورام ونشاطاتها البيولوجية على صحة الإنسان

2019 ◽  
Vol 3 (1) ◽  
Author(s):  
Hassan Mahmoud Moheisen
Keyword(s):  
Human Health ◽  
Biological Activities ◽  
Folk Medicine ◽  
Human Colon ◽  
Biological Properties ◽  
Present Review ◽  
Isolation And Identification ◽  
Human Colon Cancer ◽  
Active Constituents ◽  
Antitumour Agents

  Flavonoids are ubiquitous in photosynthesising cells and are commonly found in fruit, vegetables, nuts, seeds, stems, flowers, tea, wine, propolis and honey. Therefore, a significant quantity is consumed in our daily diet. These flavonoids are variously associated with the sensory and nutritional quality of our plant foods. For centuries, preparations containing these compounds as the principal physiologically active constituents have been used to treat human diseases. There have been many bioassay guided searches for cytotoxic antitumour agents in plants especially those known to be used in folk medicine for this purpose. This has led to the isolation and identification of quite a large number of active constituents from all the diferent flavonoid classes, e.g. catechins, flavans, dihydrochalcones, chalcones, flavanones, dihydro- flavonols, flavones, biflavonoids and flavonol. The purpose of the present review is to discuss recent developments in the biochemistry and medicinal aspects of the flavonoids. It is already well established that flavonoids make some contribution to disease resistance. Perhaps the most active area of flavonoid research at the present time is in the possible medicinal contribution that flavonoids make to human health, It is well known that some flavonoids can act as anti-spasmolytic agents, antibacterial activity, hepatoprotective agents and prevention of malaria. Recent research on the biological properties of flavonoids will therefore be a further subject of the present review. The activity of 17- β- estradiol, for example, have a pharmacologicalefficacy, at optimal concentrations, which is equivalent to the natural hormone. The compounds: 4´,7´´- di- O- methylamentofavone and 7´´- O- methylrobustafavone, were significantly cytotoxic against human cell lines including breast, lung, colon and prostate cancer, fibrosarcoma, glibostoma, oral epidermoid carcinoma and leukemia. Amongst the favonols, quercetagetin 6,7,3´ ,4´- tetramethyl ether, was found to show significant cytotoxicity against murine leukaemia, human non- small cell lung cancer, human colon cancer, and KB tumour cells.  

An Overview on Pyranocoumarins: Synthesis and Biological Activities

2020 ◽  
Vol 23 (24) ◽  
pp. 2679-2721 ◽  
Author(s):  
Evangelia-Eirini N. Vlachou ◽  
Konstantinos E. Litinas
Keyword(s):  
Organic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Properties ◽  
Pyran Ring ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal ◽  
Anti Hiv

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.

Helenalin - A Sesquiterpene Lactone with Multidirectional Activity

2019 ◽  
Vol 20 (4) ◽  
pp. 444-452 ◽  
Author(s):  
Joanna Drogosz ◽  
Anna Janecka
Keyword(s):  
Sesquiterpene Lactone ◽  
Molecular Mechanisms ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Folk Medicine ◽  
Biological Properties ◽  
Pathological Conditions ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Minor Injuries

Sesquiterpene lactones, secondary metabolites of plants, present in a large number of species mostly from the Asteracea family, are used in the traditional medicine of many countries for the treatment of various pathological conditions. They exert a broad range of activities, including antiinflammatory, anti-bacterial and anti-cancer properties. The best-known sesquiterpene lactones which are already used as drugs or are used in clinical trials are artemisinin, thapsigargin and parthenolide. Yet another sesquiterpene lactone, helenalin, an active component of Arnica montana, known for its strong anti-inflammatory activity, has been used for centuries in folk medicine to treat minor injuries. Unfortunately, helenalin’s ability to cause allergic reactions and its toxicity to healthy tissues prevented so far the development of this sesquiterpene lactone as an anticancer or anti-inflammatory drug. Recently, the new interest in the biological properties, as well as in the synthesis of helenalin analogs has been observed. This review describes helenalin's major biological activities, molecular mechanisms of action, its toxicity and potential for further research.

Indazole as a Privileged Scaffold: The Derivatives and their Therapeutic Applications

2020 ◽  
Vol 20 ◽  
Author(s):  
Jinling Qin ◽  
Weyland Cheng ◽  
Yong-Tao Duan ◽  
Hua Yang ◽  
Yongfang Yao
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Vital Role ◽  
Drug Molecules ◽  
Structure Activity ◽  
Privileged Scaffold ◽  
Future Direction ◽  
Relationship Of ◽  
Anti Hiv ◽  
Clinical Drug

Background: Heterocyclic compounds, also called heterocycles, are a major class of organic chemicalcompound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. Methods: A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. Results: The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. Conclusion: This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compoundswhere the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.

Heterocyclic Compounds Bearing Triazine Scaffold and Their Biological Significance: A Review

2020 ◽  
Vol 20 (1) ◽  
pp. 4-28
Author(s):  
Tarawanti Verma ◽  
Manish Sinha ◽  
Nitin Bansal
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Significance ◽  
Resonance Energy ◽  
Weak Bases ◽  
Anti Cancer ◽  
Interesting Class ◽  
Synthetic Derivatives ◽  
Derivatives Of

Benzene is a six-membered hydrocarbon ring system and if three carbon-hydrogen units of benzene ring are replaced by nitrogen atoms then triazine is formed. Triazines are present in three isomeric forms 1,2,3- triazine, 1,2,4-triazine, and 1,3,5-triazine according to the position of the nitrogen atom. These are weak bases having weaker resonance energy than benzene, so nucleophilic substitution is preferred than electrophilic substitution. Triazine is an interesting class of heterocyclic compounds in medicinal chemistry. Numerous synthetic derivatives of triazine have been prepared and evaluated for a wide spectrum of biological activities in different models with desired findings such as antibacterial, antifungal, anti-cancer, antiviral, antimalarial, antiinflammatory, antiulcer, anticonvulsant, antimicrobial, insecticidal and herbicidal agents. Triazine analogs have exposed potent pharmacological activity. So, triazine nucleus may be considered as an interesting core moiety for researchers for the development of future drugs.

scholarly journals Essential oils biological activity of the Lippia alba (Verbenaceae) shrub

2020 ◽  
Vol 68 (1) ◽  
Author(s):  
Mailen Ortega Cuadros ◽  
Emma E Acosta de Guevara ◽  
Ailen D Molina Castillo ◽  
Clara Gutiérrez Castañeda ◽  
Glorismar Castro Amarís ◽  
...  
Keyword(s):  
Biological Activity ◽  
Essential Oils ◽  
Biological Activities ◽  
Biological Properties ◽  
Research Groups ◽  
Lippia Alba ◽  
Sedative Effects ◽  
Aromatic Species ◽  
Meta Analyses ◽  
The Relationship

Introduction: Lippia alba is an aromatic species belonging to the Verbenaceae family. Its essential oils have been used in different industries, because of its biological properties. Objective: Identify the perspectives of the biotechnological applications of Lippia alba essential oils. Methodology: A scoping review was conducted on the biological activity of Lippia alba essential oils registered until October, 2018 in EBSCO, Embase, Scopus, and Lilacs databases. Results: Chemotypes I and III have been reported for different biological activities from the evaluations performed on microorganisms, fish, arthropods, small mammals, and cell lines; fundamentally associated with antibacterial, antifungal, cytotoxic, antioxidant, and sedative effects, among others. Records focused mainly on the health, fishing industry, and agrifood sectors. Conclusion: Studies on the effect of essential oil are promising, but do not reflect a continuity of the research toward prototypes or finished commercial products. Research groups must unify evaluation methodologies and include in all studies the relationship between phytochemical and biological activity for the meta-analyses to be possible. Likewise, they must join efforts through the National System for Agricultural Innovation (SNIA, for the term in Spanish) to generate finished products that impact upon society and facilitate progress in the country’s bio-economy.

scholarly journals 2-Acetylbenzimidazole: a Valuable Synthon for the Synthesis of Biologically Active Molecules

2020 ◽  
Vol 11 (4) ◽  
pp. 11562-11591
Keyword(s):  
Heterocyclic Compounds ◽  
Heterocyclic System ◽  
Biological Activities ◽  
Biologically Active ◽  
Online Search ◽  
Convenient Synthesis ◽  
Anti Cancer ◽  
Pharmacological Interest ◽  
Main Motive ◽  
Biological Aspects

Benzimidazole is an important moiety from a medicinal chemistry perspective due to its various biological activities such as antimicrobial, anti-cancer, anti-diabetic, anti-Alzheimers, and anti-inflammatory, etc. 2-acetylbenzimidazole is exploited to obtain various heterocyclic compounds of pharmacological interest. This review's main motive is to present the literature on 2-acetylbenzimidazole chemistry and provide valuable and up-to-date information for its applications. The present review is carried out by compiling literature from 1964 to 2020 concerning the synthesis and biological aspects of various heterocyclic compounds derived from 2-acetylbenzimidazole. Literature was collected from various online search engines viz. Google Scholar, PubMed, Science Direct, Core, and Semantic scholar. 2-acetylbenzimidazole has been successfully employed as a synthon to obtain heterocyclic system viz. oxirane, pyrazoline, thiazole, pyrazole, isoxazoline, isoxazole, pyridine, pyrimidine, thiazine, diazepine, and other miscellaneous rings. 2-acetylbenzimidazole has shown promise for the convenient synthesis of various heterocyclic compounds. The reactions can be carried out on various reactive sites of 2-acetylbenzimidazole, which are the carbonyl group and the amino group. This review will help to explore various heterocyclic compounds and particularly in the synthesis of biologically useful compounds.

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