Benzofuran: A Key Heterocycle - Ring Closure And Beyond

2020 ◽  
Vol 17 (3) ◽  
pp. 224-276
Author(s):  
Andiappan Lavanya ◽  
Kilambi Narasimhan ◽  
Vediappen Padmini
Keyword(s):  
Biological Activities ◽  
Extraction Process ◽  
Ring Closure ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Synthetic Materials ◽  
Privileged Scaffold ◽  
Medicinal Properties ◽  
Anti Inflammatory ◽  
Anti Hiv

: The benzofuranyl motif present in compounds exhibits various medicinal properties and non-drug applications. These derivatives are naturally occurring compounds or synthetic materials, which cover a broad spectrum of pharmacological activities like anti-inflammatory, anti-diabetic, anti- depressant, anti-HIV, anti-microbial, anti-proliferative, anti-convulsant, cytotoxic, analgesic, etc. Few of the commercially interesting compounds from this class are, ailanthoidol (anti-inflammatory), amiodarone, dronedarone, celivarone (anti-arrhythmic), bufuralol (muscular airways relaxant), morphine, 5-(2-aminopropyl)benzofuran; 5-APB, 6-(2-aminopropyl)benzofuran; 6-APB (CNS), rifampicin (antibiotic), etc., whereas, some of the non-drug applications are in perfumery industry (bergapten) and as tannin activators in sunscreen preparations (psoralen, 8-methoxypsoralen, and angelicin). Considering these interesting biological activities and commercial utilities, a review on the synthetic aspects of this privileged scaffold was attempted. For the benefit of natural product-based drug discovery, available sources of these derivatives, extraction process and reported biological activities have also been outlined in this review.

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.

scholarly journals Arylnaphthalene lactones: structures and pharmacological potentials

2021 ◽  
Author(s):  
Soyoung Park ◽  
Seungsu Kim ◽  
Dongyun Shin
Keyword(s):  
Drug Discovery ◽  
Medicinal Plants ◽  
Biological Activities ◽  
Structural Diversity ◽  
Structural Features ◽  
Type I ◽  
Type Ii ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Anti Hiv

AbstractNatural arylnaphthalene lactones are representative lignans that are found in various dietary and medicinal plants. Their unique structural features and significant pharmacological activity have attracted considerable attention from both synthetic and medicinal chemists. Owing to their unique structural features such as relative rigid tetracyclic skeleton, structural diversity of more than five substituents, and no chiral center, arylnaphthalene lactones are recognized as a valuable scaffold for drug discovery, in addition to their significant pharmacological activities. This review covers the structures and isolation of all naturally occurring arylnaphthalene lactone congeners reported. Based on the aryl substituents, they were categorized as Type I and Type II and further classified according to the oxidation state of the ring and glycosylation level. Special attention has been paid to natural arylnaphthalene lactones owing to their broad spectrum of biological activities such as cytotoxic, antiplatelet, antiviral, anti-HIV, antifungal, neuroprotective, and anti-inflammatory properties. All the products were reorganized based on their biological activities, and selected data are presented.

scholarly journals RECENT STRATEGIES FOR EFFICIENT SYNTHESIS AND BIOLOGICAL ACTIVITIES OF COUMARIN-CHALCONE DERIVATIVES

2020 ◽  
pp. 28-37
Author(s):  
SATHISH KUMAR KONIDALA ◽  
VIJAY KOTRA
Keyword(s):  
Antimalarial Activity ◽  
Biological Activities ◽  
Clinical Applications ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Huge Number ◽  
Pharmacological Activities ◽  
Chalcone Derivatives ◽  
Naturally Occurring ◽  
Anti Inflammatory

Coumarins and chalcones are potential pharmacological and biologically active molecules obtained from natural source. Coumarins have predominant pharmacological activities such as antidiabetic, antitumor, and anti-inflammatory activity. Chalcones are also one of the naturally occurring pharmacologically vital molecules with different activities such as anti-inflammatory, antitumor, antimicrobial, and antimalarial activity. Literature reveals that a huge number of coumarinyl chalcone derivatives have various pharmacological activities. Coumarinyl chalcone derivatives gained more prominence due to their significant biological activities. This work explains the current information about synthesis techniques, pharmacological importance, and clinical applications of coumarinyl chalcone derivatives.

Development and characterization of electrospun curcumin-loaded antimicrobial nanofibrous membranes

2020 ◽  
pp. 004051752092551
Author(s):  
Javeed A Awan ◽  
Saif Ur Rehman ◽  
Muhammad Kashif Bangash ◽  
Fiaz Hussain ◽  
Jean-Noël Jaubert
Keyword(s):  
Biological Activities ◽  
Research Work ◽  
Medical Applications ◽  
Electrospinning Technique ◽  
Naturally Occurring ◽  
Wide Range ◽  
Nanofibrous Membranes ◽  
Antimicrobial Barrier ◽  
Anti Hiv

Curcumin is a naturally occurring hydrophobic polyphenol compound. It exhibits a wide range of biological activities such as antibacterial, anti-inflammatory, anti-carcinogenic, antifungal, anti-HIV, and antimicrobial activity. In this research work, antimicrobial curcumin nanofibrous membranes are produce by an electrospinning technique using the Eudragit RS 100 (C19H34ClNO6) polymer solution enriched with curcumin. The morphology and chemistry of the membrane are analyzed using scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Kirby Bauer disk diffusion tests are carried out to examine the antibacterial effectiveness of the membrane. Experimental results show that the nanofibers produced are of uniform thickness morphology and curcumin is successfully incorporated into the nanofibrous mat, while no chemical bonding was observed between curcumin and the polymer. The antimicrobial curcumin nanofibrous membranes can be effectively applied as antimicrobial barrier in a wide variety of medical applications such as wound healing, scaffolds, and tissue engineering.

Pharmacologic activities of 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazines as a privileged scaffold in drug development

2021 ◽  
Vol 21 ◽  
Author(s):  
Zahra Zakeri Khatir ◽  
Hamid Irannejad
Keyword(s):  
Biological Data ◽  
Pharmacological Activities ◽  
Drug Candidates ◽  
Structure Activity ◽  
Wide Range ◽  
Privileged Structure ◽  
Triazine Derivatives ◽  
Privileged Scaffold ◽  
Substituted 1 ◽  
Anti Hiv

: 1, 2, 4-Triazine derivatives have received much attention due to their multifunctional nature, especially in diverse pharmacological properties as well as a key fragment in many drug candidates. Introduction of a vicinal 5, 6-diaryl/heteroaryl moiety on the 1, 2, 4-triazine ring has attracted plentiful attention in the field of medicinal chemistry. 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazine is as a prominent scaffold in many drug candidates which has shown a wide range of pharmacological activities such as anti-diabetic, antifungal, anti-inflammatory, anticancer, anti-HIV, neuroprotective, anticonvulsant, anti- Alzheimer, anti-Parkinson and antioxidant. In this review, we have discussed synthesis, various pharmacological activities of 5, 6-diaryl/heteroaryl-3-substituted-1, 2, 4-triazines, their structure-activity relationship (SAR), pharmacophoric elements and their mechanism of action reported in the published articles during 2000-2019. Evaluation of compounds by PAINS filtering tool was accomplished and showed that this versatile structure could be considered as a privileged structure. Compilation of the biological data confirmed that the position 3 of the 1,2,4-triazine is a key location to determine the affinity and selectivity of the 5,6-diaryl/heteroaryl-3-substituted-1, 2, 4-triazines towards different biologic targets. Specific geometrical and thermodynamic characters of this motif have prompted it as a frequent hitter.

scholarly journals Harnessing the medicinal properties of Cussonia barteri Seem. (Araliaceae) in drug development. A review

2018 ◽  
Vol 64 (3) ◽  
pp. 50-61 ◽  
Author(s):  
Ighodaro Igbe ◽  
Osaze Edosuyi ◽  
Agbonlahor Okhuarobo
Keyword(s):  
Drug Development ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Stem Bark ◽  
Deciduous Tree ◽  
Drug Candidates ◽  
Medicinal Properties ◽  
Phytochemical Constituents ◽  
Anti Inflammatory ◽  
Novel Drug

Summary Cussonia barteri Seem (Araliaceae) is a deciduous tree growing in savannah of Africa. Ethnomedicinally, it is used in Africa as an analgesic, anti-malarial, anti-inflammatory, anti-anaemic, anti-diarhoea, anti-poison, ani-pyschotic and anti-epileptic agent. This review provides a brief summary on the phytochemical screenings, ethnomedicinal and pharmacological applications of various parts of C. barteri. Leaves, stem bark and seed of C. barteri have been shown to be rich in saponins, flavonoids, phenols, sugars and alkaloids. Some of these constituents have been isolated and elucidated from C. barteri. Several compounds isolated from plant include triterpenes, saponins, polyenyne and quinic esters. Phytochemical constituents are also partly responsible for biological activities of C. barteri. Extracts and components isolated from the plant have demonstrated neuropharmacological, anti-larvicidal, anti-microbial, anti-inflammatory and antioxidant activities. Overall, the insights provided by this review reinforce the potential of C. barteri for drug development and create the need for further scientific probe of constituents of the plant with the aim of developing novel drug candidates.

scholarly journals Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review

2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi
Keyword(s):  
Nitrogen Atom ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Cardiovascular Agents ◽  
Anti Hiv ◽  
Biological And Pharmacological Activities

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.

scholarly journals Recent Advances in Synthesis of 4-Arylcoumarins

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2417 ◽  
Author(s):  
Jong-Wha Jung ◽  
Nam-Jung Kim ◽  
Hwayoung Yun ◽  
Young Han
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Metal Catalysis ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Formation Type ◽  
Privileged Scaffold ◽  
Acid Catalyzed ◽  
A Minor ◽  
Synthetic Approaches

4-Arylcoumarins (4-aryl-2H-1-benzopyran-2-one), also known as neoflavones, comprise a minor subclass of naturally occurring flavonoids. Because of their broad-spectrum biological activities, arylcoumarins have been attracting the attention of the organic and medicinal chemistry communities, and are considered as an important privileged scaffold. Since the development of Pechmann condensation, a classical acid-catalyzed condensation between phenol and β-keto-carboxylic acid, several versatile and efficient synthetic approaches for 4-arylcoumarins have been reported. This review summarizes recent advances in the synthesis of the 4-arylcoumarin scaffold by classifying them based on the final bond-formation type. In particular, synthetic methods executed under mild and highly efficient conditions, such as solvent-free reactions and transition metal catalysis, are highlighted.

PHYTOCHEMICAL, PHARMACOLOGICAL SCREENING AND IMPORTANCE OF MARSDENIA TENACISSIMA: A REVIEW

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (4) ◽  
pp. 7-22
Author(s):  
Mayur Porwal ◽  
◽  
Arvind Kumar ◽  
Kamal K. Maheshwari ◽  
Najam A. Khan ◽  
...  
Keyword(s):  
Heart Disease ◽  
Skin Disease ◽  
Recent Literature ◽  
Biological Activities ◽  
Intermittent Fever ◽  
Pharmacological Activities ◽  
Phytochemical Constituents ◽  
Pharmacological Screening ◽  
Anti Hiv ◽  
Marsdenia Tenacissima

In conventional methods of medication, Marsdenia tenacissima (family: Apocynaceae) is used in the treatment of scurvy, urinary diseases, arthritis, heart disease, skin disease, pruritus, vomiting and intermittent fever. Estimation of biological activities confirmed that M. tenacissima plant shows antipyretic, antioxidant, anticancer and anti-HIV activities. This assessment presents the phytochemical constituents, traditional importance and pharmacological activities accounted for the plant in recent literature and it will be supportive to explore incisive information about M. tenacissima for the researchers.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

Sign in / Sign up

Export Citation Format

Share Document