Quinoxaline: A chemical moiety with spectrum of interesting biological activities

2021 ◽  
Vol 21 ◽  
Author(s):  
Aastha Sharma ◽  
Aakash Deep ◽  
Minakshi Gupta Marwaha ◽  
Rakesh Kumar Marwaha
Keyword(s):  
Antibacterial Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Growth Promoter ◽  
Organic Reaction ◽  
Acid Inhibitor ◽  
Drug Molecules ◽  
Quinoxaline Derivatives ◽  
Different Types ◽  
Heterocyclic Moiety

: Quinoxaline (C8H6N2), commonly called 1,4-diazanaphthalene, 1,4-benzodiazine, or benzopyrazine, is a very potent nitrogenous heterocyclic moiety consisting of a benzene ring fused with the pyrazine ring. A number of different methods for the synthesis of quinoxaline derivatives have been reported in the literature, but the most effective method, commonly used for the synthesis of quinoxaline analogues involves the condensation of substituted o-phenylenediamines with 1, 2- dicarbonyl compounds in the presence of different catalyst(s). The presence of different types of catalysts and their concentration affects the overall yield of the product. Quinoxaline not only plays an important role as an organic reaction intermediate but also has a wide spectrum of interesting biological activities viz. antibacterial, antifungal, anticancer, anti-inflammatory, antiviral, and antiprotozoal activity, etc. Some commercially available drug molecules containing quinoxaline moiety are echinomycin (as antibacterial, antineoplastic, and nucleic acid inhibitor), triostins (cyclic desipeptide as an antibacterial agent), dioxidine and mequindox (as antibacterial agents), carbadox (controlling swine dysentery), desoxycarbadox (as swine growth promoter) and panadipion (as hepatoprotective agent), etc. A large number of quinoxaline analogues possessing different biological activities and their synthetic procedures have been patented worldwide.

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.

Current developments in the Pyran-Based Analogues as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Lovekesh Mehta ◽  
Garima Kapoor ◽  
Pooja A. Chawla
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Anticancer Compounds ◽  
Appropriate Treatment ◽  
Anti Cancer ◽  
Privileged Structure ◽  
Different Types

: Heterocyclic compounds offer an enormous area for new lead molecules for drug discovery. Till today, efforts are being continuously made to find appropriate treatment for the management of the deadly disease of cancer. Amongst the large number of heterocycles that are found in nature, heterocycles having oxygen obtained noteworthy attention due to their distinctive and pharmacological activities.‘Pyran’ is one of the most significant non-aromatic, six-membered ring composed of one oxygen atom and five carbon atoms. It is considered a privileged structure since pyran and its related derivatives exhibit a wide spectrum of biological activities. Pyran derivatives are found to have excellent anti-cancer properties against various types of cancer. The present review focussed on the current advances in different types of pyran-based derivatives as anti-cancer agents. Various in-vitro (cell based testing), in-vivo (animal based testing) models as well as molecular docking along with results are also covered. A subsection describing briefly natural pyran containing anticancer compounds is also incorporated in the review.

scholarly journals Pharmaceutical Drug Polymorphism: A Case Study of Three Novel Drugs

2014 ◽  
Vol 70 (a1) ◽  
pp. C544-C544
Author(s):  
Rajni Kant
Keyword(s):  
Crystal Engineering ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Solvent System ◽  
Ideal Condition ◽  
X Rays ◽  
Pharmaceutical Drug ◽  
Drug Molecules ◽  
Drug Polymorphism ◽  
High Level

Polymorphism is more widespread in pharmaceutical solids, with estimates of 30-50% in drug-like molecules, compared to 4-5% polymorphic crystals in the Cambridge Structural Database (Nangia, 2007). Most of the drug molecules are formulated and marketed in crystalline form and many of these are highly functionalized and can self-organize in several ways in the solid state with nearly the same lattice energies. Though a lot of work is going on in the field of pharmaceutical drug polymorphism and its possible application in the field of crystal engineering, yet there are difficulties in getting polymorphs of many important molecules. The present work deals with a comparative crystallographic study on the existing polymorphic forms of three medicinally important molecules, Aspirin, Paracetamol and Norfloxacin which are known to have a wide spectrum of medicinal activities. Broadly, the present study accounts for the following observations: (i) Choice of the solvent system, its purity and its reaction mechanism with solute under ideal condition of growth/crystallization. (ii) The interaction of grown material with X-rays should be very healthy in the sense that maximum number of planes in a given crystal should diffract the incoming X-ray beam. This aspect is once again related to quality single crystal growth. Fairly good interaction of a compound with X-rays leads to better refined structure, yielding a very high level of confidence between the chemical and computed structure. (iii) Analysis of a molecule's ability to exhibit biological activities by employing some suitable empirical and clinical modes. (iv) Most of physical properties of a grown material depend on how the molecules have been packed in the unit cell and how the derived knowledge of intra and intermolecular interactions is applied for engineering a crystal of choice.

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.

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.

Anthocyanins As Modulators of Cell Redox-Dependent Pathways in Non-Communicable Diseases

2020 ◽  
Vol 27 (12) ◽  
pp. 1955-1996 ◽  
Author(s):  
Antonio Speciale ◽  
Antonella Saija ◽  
Romina Bashllari ◽  
Maria Sofia Molonia ◽  
Claudia Muscarà ◽  
...  
Keyword(s):  
Human Health ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Antioxidant Defenses ◽  
Noncommunicable Diseases ◽  
Protective Effects ◽  
Pathological Conditions ◽  
Chronic Pulmonary Diseases ◽  
Underlying Mechanisms

: Chronic Noncommunicable Diseases (NCDs), mostly represented by cardiovascular diseases, diabetes, chronic pulmonary diseases, cancers, and several chronic pathologies, are one of the main causes of morbidity and mortality, and are mainly related to the occurrence of metabolic risk factors. Anthocyanins (ACNs) possess a wide spectrum of biological activities, such as anti-inflammatory, antioxidant, cardioprotective and chemopreventive properties, which are able to promote human health. Although ACNs present an apparent low bioavailability, their metabolites may play an important role in the in vivo protective effects observed. : This article directly addresses the scientific evidences supporting that ACNs could be useful to protect human population against several NCDs not only acting as antioxidant but through their capability to modulate cell redox-dependent signaling. In particular, ACNs interact with the NF-κB and AP-1 signal transduction pathways, which respond to oxidative signals and mediate a proinflammatory effect, and the Nrf2/ARE pathway and its regulated cytoprotective proteins (GST, NQO, HO-1, etc.), involved in both cellular antioxidant defenses and elimination/inactivation of toxic compounds, so countering the alterations caused by conditions of chemical/oxidative stress. In addition, supposed crosstalks could contribute to explain the protective effects of ACNs in different pathological conditions characterized by an altered balance among these pathways. Thus, this review underlines the importance of specific nutritional molecules for human health and focuses on the molecular targets and the underlying mechanisms of ACNs against various diseases.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

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.

Medicinal Chemistry of Alternative Therapeutics: Novelty and Hopes with Genus Ammannia

2019 ◽  
Vol 19 (10) ◽  
pp. 784-794 ◽  
Author(s):  
Harish C. Upadhyay
Keyword(s):  
Traditional Medicine ◽  
Biological Activities ◽  
World Health ◽  
Biologically Relevant ◽  
Traditional Medicines ◽  
Drug Molecules ◽  
Health Organization ◽  
Tract Infections ◽  
Pharmacologically Active ◽  
Herbal Formulations

The plants have formed the basis of folklore remedy since the beginning of human civilization. The cumulative human endeavor and experience over a period of thousands of years developed into well to organize traditional medicine systems viz. Ayurvedic, Unani, Chinese amongst others. Across the world, traditional medicine is either the mainstay of health care or serves as a complement to modern drugs. In view of worldwide use of traditional medicines, World Health Organization launched ‘WHO-Traditional Medicine Strategy 2014-2023’ for the development of strong policies regarding knowledge-base, safety, quality-control and effectiveness of traditional/alternative therapeutics for national health systems. Besides their use in traditional medicine, plants have always been a good source of modern drug/pharmacologically active molecules. More than half of the modern pharmaceuticals are either plant isolates or their derivatives. The plant-based drugs are not only effective, but have better compatibility with human biological systems because of more biologically relevant chemistry, hence lesser side effects. Some of the species of genus Ammannia (Lythraceae) have been reported for their magical medicinal values. Many herbal formulations containing Ammannia spp. have been patented for treatment of serious diseases/disorders like cancer, spinal disease, human female infertility, chronic tonsillitis, pelvic inflammatory disease, treatment of bladder stones, urinary tract infections, dermatitis etc. The uses of Ammannia spp. in traditional medicine have been further verified by the biological activities of their extracts as well as isolation of bioactive phytomolecules. The current review provides details about Ammannia spp.; its use in folklore remedy, herbal formulations, biological activities of extracts, isolation of bioactive phytomolecules and SAR study of semi-synthetic derivatives to analyze the possibility of new drug molecules of plant origin.

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