Synthetic Pathways to Substituted Coumarins: A Comprehensive Guide | Book Publisher International

 

Coumarins, a ubiquitous class of natural benzopyrones, are a foundational scaffold in medicinal chemistry due to their extensive array of biological activities. This report details the advanced synthetic strategies for generating substituted coumarins, with a particular focus on the construction of angular and linear furo- and pyranocoumarin derivatives. Key synthetic transformations discussed include the Claisen rearrangement, Wittig reaction, selenium dioxide oxidation, sodium borohydride reduction, Reformatsky reaction, and Grignard reaction. Each methodology is examined for its specific contribution to the precise formation and functionalization of these complex heterocyclic systems. The report emphasises the pharmaceutical importance of angular and linear furo- and pyranocoumarin derivatives, highlighting their broad-spectrum therapeutic applications, such as anticancer, anti-inflammatory, antimicrobial, and neuroprotective effects. It also addresses the critical role of structure-activity relationships in guiding synthetic design and the ongoing efforts to overcome challenges like drug resistance and optimising bioavailability, underscoring the continuous evolution of coumarin chemistry for therapeutic innovation.

 

Author(s) Details

Dr. Ranjit Kumar Shit
Department of Chemistry, Vidyasagar College (Calcutta University), Kolkata, India.

 

Dr. Nitai Chand Sinha
Department of Chemistry, Sarat Centenary College (Burdwan University), India.

 

 

Please see the book here:- https://doi.org/10.9734/bpi/mono/978-81-991703-9-1

Synthetic Pathways to Substituted Coumarins: A Comprehensive Guide | Book Publisher International

 

Coumarins, a ubiquitous class of natural benzopyrones, are a foundational scaffold in medicinal chemistry due to their extensive array of biological activities. This report details the advanced synthetic strategies for generating substituted coumarins, with a particular focus on the construction of angular and linear furo- and pyranocoumarin derivatives. Key synthetic transformations discussed include the Claisen rearrangement, Wittig reaction, selenium dioxide oxidation, sodium borohydride reduction, Reformatsky reaction, and Grignard reaction. Each methodology is examined for its specific contribution to the precise formation and functionalization of these complex heterocyclic systems. The report emphasises the pharmaceutical importance of angular and linear furo- and pyranocoumarin derivatives, highlighting their broad-spectrum therapeutic applications, such as anticancer, anti-inflammatory, antimicrobial, and neuroprotective effects. It also addresses the critical role of structure-activity relationships in guiding synthetic design and the ongoing efforts to overcome challenges like drug resistance and optimising bioavailability, underscoring the continuous evolution of coumarin chemistry for therapeutic innovation.

 

Author(s) Details

Dr. Ranjit Kumar Shit
Department of Chemistry, Vidyasagar College (Calcutta University), Kolkata, India.

 

Dr. Nitai Chand Sinha
Department of Chemistry, Sarat Centenary College (Burdwan University), India.

 

Please see the link:- https://doi.org/10.9734/bpi/mono/978-81-991703-9-1

Meglumine Catalyzed Efficient Synthesis of Coumarin Derivatives | Chapter 10 | Recent Developments in Chemistry and Biochemistry Research Vol. 4

It has been found that meglumine a biodegradable basic organo-compound is an efficient catalyst for the C-O bond formation between 4-hydroxycoumarin and arylacetate, under mild reaction conditions at room temperature with high product yield. Various 4-(1-aryl ethoxy)-2H-chromen-2-ones are obtained in good to excellent yields using this method.

 

Author (s) Details

 

S. Aravind
Department of Chemistry, University College of Science, Saifabad, Osmania University, Hyderabad, Telangana, India.

 

K. A. Emmanuel
Department of Chemistry, Y.V.N.R. Government Degree College, Kaikaluru, A.P., India.

 

T. Somasekhar
Department of Freshmen Engineering, St. Martin’s Engineering College, Hyderabad, Telangana, India.

 

B. S. N. Murthy
Department of Chemistry, Sir C R Reddy College, Eluru, Andhra Pradesh, India.

Ch.Bhuvaneswari
Department of Chemistry, Adikavi Nannaya University, Rajamahendravaram, A.P., India.

 

Please see the book here:- https://doi.org/10.9734/bpi/rdcbr/v4/1211

Coumarin in Brazilian cachaça stored in barrels of Amburana cearensis | Chapter 8 | Current Perspectives in Agriculture and Food Science Vol. 5

 The purpose concerning this chapter search out determine in what way or manner closely cachaça continued in amburana barrels adhered to the palpable coumarin content limit set out by Brazilian and worldwide law. In this phase, the coumarin content of twelve marketing cachaças, whose labels specify depository in amburana wood barrels, was checked. The phenolic chemical coumarin (1,2-benzopyrone) is arisen plants. In addition to being widely utilized cruel medicine, it is further employed as a bioactive factor in nutraceutical foods in addition to an odorant in food, drinks, cosmetic, and fragrance. The drink known as cachaça is created in Brazil by distilling sugarcane juice that has sustained fermentation. International well-being organizations warn a daily use cap of 0.1 mg/kg owing to the feasibility of hepatotoxicity and other negative results in more susceptible things. Brazilian law has set a limit of 10 mg/kg for coumarin in alcoholic beverages, following a all-encompassing trend. The average result for nine samples picked as most representative (18.0 ± 7.0 mg/L) was above the allowable established limit. The results of three samples were ignored, two for being much below (0.6 and 0.8 mg/L, individually); and the third, for being much over the average (45.1 mg/L), accompanying poor auditory quality and not acceptable for commercialization.  It was concluded that skilled is a need for more rigor in the labeling of the wood variety (Amburana cearensis) used in the produce of amburana barrels and for more effective control of the coumarin content moved to the cachaça during depository in this forest.

Author(s) Details:

Amazile Biagioni Maia,
Laboratório LABM, Brasil.

Lorena Simão Marinho,
Laboratório LABM, Brasil.

Lucas Oliveira Tonidandel,
Universidade Federal de Minas Gerais, Brasil.

Frederico Marx Brom Carneiro,
Universidade UniBH, Brasil.

Elaine Cristina da Conceição,
Laboratório LABM, Brasil.

Bárbara Dias Machado,
Laboratório LABM, Brasil.

Please see the link here: https://stm.bookpi.org/CPAFS-V5/article/view/11750

Molecular Docking and Pharmacokinetic Prediction Studies of Novel Coumarin Derivatives as Arylamine N- acetyltransferase 2 Inhibitors | Chapter 5 | Current Aspects in Pharmaceutical Research and Development Vol. 2

 Many medicines and carcinogens are detoxified by arylamine N-acetyltransferases, which are xenobiotic-metabolizing enzymes. It can bioactivate several recognised carcinogens by catalysing the N- or O-acetylation of different arylamine and heterocyclic amine substrates. The presence of NATs in the body has significant implications for an individual's vulnerability to drug-induced toxicity and malignancy. The goal of this work is to use AutoDock 4.0.1 software to analyse the affinity of computationally created coumarin derivatives on NAT2 and evaluate the interactions between the target compounds and the enzyme's amino acid residues. Molinspiration was used to investigate the molecular characteristics of created molecules. All compounds followed the Lipinski rule of five, indicating that they exhibit outstanding drug similarity qualities and are better suited for use as an orally administered medication. The pkCSM software was used to predict the pharmacokinetics of coumarin derivatives in this investigation. The ADMET attributes prediction findings revealed that all developed compounds have good metabolic properties and no evident toxicity. Among the proposed compounds, 3-dibutyl-7-hydroxy-4-oxo-2-chlrobenzyl -4H chromene -8-carbaldehyde (compound 5) had the highest binding energy (-9.08). These results indicate that the intended coumarin compounds are effective NAT2 inhibitors.

Author(s) Details

Shiny George
Department of Pharmaceutical Chemistry, Hindustan College of Pharmacy, Kottayam, Kerala, India.

P. K. Sujith
Department of Pharmacology, Hindustan College of Pharmacy, Kottayam, Kerala, India.

Meena Chandran
Department of Pharmaceutical Chemistry, St James College of Pharmaceutical Sciences, Thrissur, Kerala, India.

Kumaran Santhalingam
Gensilico Biosolutions, Chengalpattu Dist, Tamilnadu, 600045, India.

View Book :- https://stm.bookpi.org/CAPRD-V2/article/view/3953