Green and Sustainable Technology: Efficient Strategy for Synthesis of Biologically Active Pyrimidine Derivatives

2021 ◽  
Vol 08 ◽  
Author(s):  
Biswa Mohan Sahoo ◽  
B.V.V Ravi Kumar ◽  
Krishna Chandra Panda ◽  
Jammula Sruti ◽  
Abhishek Tiwari ◽  
...  
Keyword(s):  
Raw Materials ◽  
Biological Activities ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Microwave Assisted Synthesis ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Sustainable Technology ◽  
Chemical Substances ◽  
Ball Milling Technique

: Green chemistry is also referred as sustainable technology which involves the design, synthesis, processing and use of chemical substances by reducing or eliminating the chemical hazards. This strategy focuses on atom economy, use of safer solvents or chemicals, use of raw materials from renewable resources, consumption of energy and decomposition of the chemical substances to non-toxic material which are eco-friendly. So, this technology is utilized for the sustainable development of novel heterocyclic scaffold like pyrimidine derivatives. Pyrimidine is a six membered heterocyclic aromatic compound with two nitrogen atoms at positions 1 and 3 in the ring system. Among the other heterocyclic compounds, pyrimidine derivatives plays major role due to their diverse promising biological activities such as antimicrobial, antifungal, anti-viral, anti-tubercular, anti-diabetic, anti-hypertensive, anticancer, anthelmintic, antioxidant, anti-epileptic, antipsychotic, anti-anxiety, antimalarial, antihistaminic, anti-parkinsonian, analgesic and anti-inflammatory etc. The various green methods used for synthesis of pyrimidine derivatives include microwave assisted synthesis, ultrasound induced synthesis, ball milling technique, grinding technique, photo-catalysis. These processes enhance the rate of the reaction which leads to high selectivity with improved product yields as compared to the conventional synthetic methods. This review is focused on the green synthesis of biologically active pyrimidine derivatives.

Green Chemistry Approaches to the Synthesis of Coumarin Derivatives

2020 ◽  
Vol 24 (1) ◽  
pp. 4-43 ◽  
Author(s):  
Maja Molnar ◽  
Melita Lončarić ◽  
Marija Kovač
Keyword(s):  
Energy Consumption ◽  
Green Chemistry ◽  
Biological Activities ◽  
Daily Basis ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Specific Class ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Coumarin Synthesis

This review is a compilation of the green synthetic methods used in the synthesis of coumarin derivatives. Coumarins are a class of compounds with a pronounced wide range of biological activities, which have found their application in medicine, pharmacology, cosmetics and food industry. Their biological activity and potential application are highly dependent on their structure. Therefore, many researchers have been performing the synthesis of coumarin derivatives on a daily basis. High demands for their synthesis often result in an increased generation of different waste chemicals. In order to minimize the utilization and generation of toxic organic substances, green synthetic methods are applied in this manner. These methods are getting more attention in the last few decades. Green chemistry methods cover a wide range of methods, including the application of ultrasound and microwaves, ionic liquids and deep eutectic solvents, solvent-free synthesis, mechanosynthesis and multicomponent reactions. All typical condensation reactions for coumarin synthesis like Knoevenagel, Perkin, Kostanecki-Robinson, Pechmann and Reformansky reactions, have been successfully performed using these green synthetic methods. According to the authors mentioned in this review, not only these methods reduce the utilization and generation of toxic chemicals, but they can also enhance the reaction performance in terms of product yields, purity, energy consumption and post-synthetic procedures when compared to the conventional methods. Due to the significance of coumarins as biologically active systems and the recent demands of reducing toxic solvents, catalysts and energy consumption, this review provides a first full literature overview on the application of green synthetic methods in the coumarin synthesis. It covers a literature search over the period from 1995-2019. The importance of this work is its comprehensive literature survey on a specific class of heterocyclic compounds, and those researchers working on the coumarin synthesis can find very useful information on the green synthetic approaches to their synthesis. There are some reviews on the coumarin synthesis, but most of them cover only specific reactions on coumarin synthesis and none of them the whole range of green chemistry methods.

1,2,3-Triazole- and Quinoline-Based Hybrids with Potent Antiplasmodial Activity

2021 ◽  
Vol 18 ◽  
Author(s):  
Isabela A. Graciano ◽  
Alcione S. de Carvalho ◽  
Fernando de Carvalho da Silva ◽  
Vitor F. Ferreira
Keyword(s):  
Antimalarial Activity ◽  
Biological Activities ◽  
Review Article ◽  
Pharmaceutical Market ◽  
Biologically Active ◽  
New Drugs ◽  
Synthetic Methods ◽  
Antiplasmodial Activity ◽  
New Chemical Entities ◽  
Active Substances

Background: Malaria is a disease causing millions of victims every year and requires new drugs, often due to parasitic strain mutations. Thus, the search for new molecules that possess antimalarial activity is constant and extremely important. However, the potential that an antimalarial drug possesses cannot be ignored, and molecular hybridization is a good strategy to design new chemical entities. Objective: This review article aims to emphasize recent advances in the biological activities of new 1,2,3-triazole- and quinoline-based hybrids and their place in the development of new biologically active substances. More specifically, it intends to present the synthetic methods that have been utilized for the syntheses of hybrid 1,2,3-triazoles with quinoline nuclei. Method: We have comprehensively and critically discussed all the information available in the literature regarding 1,2,3-triazole- and quinoline-based hybrids with potent antiplasmodial activity. Results: The quinoline nucleus has already been proven to lead to new chemical entities in the pharmaceutical market, such as drugs for the treatment of malaria and other diseases. The same can be said about the 1,2,3-triazole heterocycle, which has been shown to be a beneficial scaffold for the construction of new drugs with several activities. However, only a few triazoles have entered the pharmaceutical market as drugs. Conclusion: Many studies have been conducted to develop new substances that may circumvent the resistance developed by the parasite that causes malaria, thereby improving the therapy currently used.

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.

Biologically active polymeric sequestrants: Design, synthesis, and therapeutic applications

2007 ◽  
Vol 79 (9) ◽  
pp. 1521-1530 ◽  
Author(s):  
Pradeep K. Dhal ◽  
Chad C. Huval ◽  
S. Randall Holmes-Farley
Keyword(s):  
Rational Design ◽  
Biological Activities ◽  
Functional Polymers ◽  
Therapeutic Agents ◽  
The Body ◽  
Biologically Active ◽  
Gi Tract ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Polymeric Drugs

In recent years, functional polymers exhibiting inherently biological activities have been receiving increasing attention as polymer-based human therapeutic agents. These polymeric drugs exhibit unique pharmaceutical properties that are fundamentally different from their traditional small-molecule counterparts. However, unlike polymeric drug delivery systems, examples of polymers possessing intrinsically therapeutic properties are relatively scarce. By virtue of their high-molecular-weight characteristics, these polymeric drugs can be confined to the gastrointestinal (GI) tract, where they can selectively recognize, bind, and remove target disease-causing substances from the body. Being confined to the GI tract and non-biodegradable, these polymeric drugs are free from toxic effects that are associated with traditional systemic drugs. This report highlights recent developments in the rational design and synthesis of appropriate functional polymers that have resulted in a number of promising polymer-based therapeutic agents, including some marketed products.

scholarly journals Phytochemical Profile and Pharmacological Activities of Water and Hydroethanolic Dry Extracts of Calluna vulgaris (L.) Hull. Herb

Plants ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 751
Author(s):  
Galyna Starchenko ◽  
Andriy Hrytsyk ◽  
Ain Raal ◽  
Oleh Koshovyi
Keyword(s):  
Raw Materials ◽  
Biological Activities ◽  
Calluna Vulgaris ◽  
Biologically Active ◽  
New Drugs ◽  
Flowering Plant ◽  
Antidepressant Effects ◽  
Phenolic Substances ◽  
Phytochemical Profile ◽  
Hydroethanolic Extract

According to the WHO data (2017), depression is the most predominant disease worldwide, with about 300 million people suffering from it, and bipolar disorder is the second most common. Therefore, it is relevant to research new medicines based on medicinal herbal raw materials with anti-anxiety and antidepressant effects. Common heather (Calluna vulgaris (L.) Hull.), a flowering plant of the Ericaceae family, is a promising species for research in this area. The aim of this study was to investigate the phytochemical profile and several biological activities of hydroethanolic dry extracts from the C. vulgaris herb. Nineteen phenolic substances were identified and quantified in the extracts by HPLC. The quantitative content of the basic groups of biologically active compounds was determined by spectrophotometry. Arbutin was dominant among the hydroquinone derivatives; chlorogenic acid among the hydroxycinnamic acids; rutin, hyperoside and quercetin-3-D-glucoside among the flavonoids; and (+)-gallocatechin and (-)-epigallocatechin among the tannin metabolites. The water and hydroethanolic extract were compared, the extract of C. vulgaris herb obtained with 70% hydroethanolic had the most pronounced anti-inflammatory, antimicrobial, anxiolytic, stress-protective, anti-anxiety and anti-depressant effects, and it is a promising substance for the development of new drugs or food supplements.

Synthesis of PF-543 Derivatives Using Simple Synthetic Methods and Their Biological Effect Analysis for the Development of Anticolorectal Cancer Agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Jitendra Shrestha ◽  
Joo-Youn Lee ◽  
Eun-Young Park ◽  
Dong Jae Baek
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Biological Activities ◽  
Docking Study ◽  
Inhibitory Effect ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Step Method ◽  
Effect Analysis ◽  
Simple Modification

Background: Sphingolipids, even in extremely low doses, regulate various physiological functions. Particularly, immune and cancer cells might be controlled by changes in the sphingosine-1-phosphate (S1P) levels, and S1P has been studied for a long time as a major target for new drug development. Sphingosine kinase (SK) phosphorylates sphingosine to produce S1P. An increase in the S1P levels promotes the growth of cancer cells. SK has 2 isoforms, SK1 and SK2, both of which are involved in the growth of cancer cells. Objective: PF-543 was developed as an SK1 inhibitor and has a non-lipid structure that differs from those of general SK inhibitors. While PF-543 has a potent SK1 inhibitory effect, it has low anticancer activity in some types of cancer cells. Therefore, the development of other PF-543 derivatives is needed. Methods: We designed a structurally simplified derivative of PF-543. To primarily demonstrate that the designed structure was biologically active, 8 derivatives were synthesized by a 2-step method using the commercial starting material, and their biological activities were evaluated. Results and Discussion: The SK1-inhibitory effects of the synthesized derivatives were not higher than that of PF-543. However, the anticancer activity and apoptotic effect of the derivatives were similar to those of PF-543, despite their fabrication from a simple modification of the PF-543 structure. In a docking study, the derivatives were found to bind SK1 in a form similar to PF-543. Conclusion: Our analogs, which are similar to PF-543, showed comparable anticancer activity, indicating that the synthesized derivatives are structurally more efficient for anticancer activity than PF-543. Therefore, our study provides important information that may be useful for developing new anticancer substances that target SK1.

Lawsone (2-hydroxy-1,4-naphthaquinone) derived anticancer agents

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Arvind Singh ◽  
Amartya Basu ◽  
Aditi Sharma ◽  
Anu Priya ◽  
Manmmet Kaur ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Lawsonia Inermis ◽  
Wide Range ◽  
Tree Leaf

Abstract 2-Hydroxy-1,4-naphthaquinone, commonly known as lawsone, represents an extremely important biologically active naturally occurring compound. It can easily be isolated from Lawsonia inermis (henna) tree leaf extract. Last decade has seen tremendous applications of lawsone as a starting component for the preparation of various organic scaffolds. Many of these synthesized scaffolds showed a wide range of biological activities including potential activities towards several cancer cell lines. This review deals with diverse synthetic methods of lawsone derived scaffolds and their screening against different anti-cancer cell lines along with promising results.

COMPARATIVE ANALYSIS OF BIOACTIVE SUBSTANCES CONTENT IN THE LEAVES AND FRUITS OF A ROWAN-TREE (SORBUS AUCUPARIA FRUCTUS) AND ASSESSMENT OF PROSPECTS IN MEDICINE AND PHARMACY

2020 ◽  
pp. 58-62
Author(s):  
Chernichkina A.D.
Keyword(s):  
Raw Materials ◽  
Wide Distribution ◽  
Biologically Active ◽  
Bioactive Substances ◽  
Plant Raw Materials ◽  
Mountain Ash ◽  
The Russian Federation ◽  
Materials Used ◽  
Active Substances ◽  
Pectin Substances

A large number of biologically active substances, organic acids, tannins, and pectin substances were detected during the study of fruits, leaves, and pulp of the fruits of mountain Ash. The content of these substances in leaves and pulp will significantly expand the arsenal of medicinal plant raw materials used. Given the wide distribution of mountain Ash in the territory of the Russian Federation, harvesting leaves from the same plants after harvesting the fruit and using pulp will make it possible to obtain new phytopreparations.

On the diagnostics of Adonis L. species (Ranunculaceae) of the Russian flora

2020 ◽  
pp. 3-14
Author(s):  
Aleksandr Luferov
Keyword(s):  
Raw Materials ◽  
Natural Populations ◽  
Structural Features ◽  
Biologically Active ◽  
Scientific Medicine ◽  
Diagnostic Features ◽  
Plant Raw Materials ◽  
Similar Chemical ◽  
Chemical Studies ◽  
Alternative Sources

The article provides brief information about cardiotonic, sedative, cytostatic, diuretic, and antibacterial effects of biologically active compounds of Adonis L. (Ranunculaceae) species. Chemical studies allowed to identify the cardiac glycosides, or cardenolides: or cardenolides: adontoxin, adonitol, adonitoxigenin, acetyldigitoxin and others. In scientific medicine, it is currently allowed to use Adonis vernalis L. Other types of Adonis have a similar chemical composition and are offered as substitutes for this official species, for example, Adonis apennina L. Many Adonis species have limited natural resources, and in some regions are rare, requiring conservation of their natural populations. The search for alternative sources of medicinal plant raw materials, based on this, is relevant. The experimental part of our research was carried out using the morphological and geographical method with the involvement of information on ecology and phenology. For the first time summarizes the diagnostic features of Adonis flora of Russian flora. Previously unknown structural features (shape and size of anthers) were identified that characterize the subgenera Adonanthe and Adonis. Taxonomic study of the genus Adonis of the Russian flora allowed us to determine its species composition, clarify its systematic affiliation, and nomenclature synonyms. 9 species were identified. Of these, 6 are perennials belonging to the subgenus Adonanthe, section Consiligo, which includes 2 subsections: Amurenses (2 species) and Vernales, which is differentiated into 2 rows: Apenninae (2 species) and Vernales (2 species). Subgenus Adonis is represented by 2 sections: Adonis (1 species) and Lophocarpa with sections Aestivales (1 species) and Dentatae (1 species). For all the considered species and varieties, the main distribution areas are given. A key has been compiled to determine the wild Adonis species distributed in Russia.

Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles

2009 ◽  
Vol 2 (1) ◽  
pp. 390-406
Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
Heterocyclic Compounds ◽  
Medical Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Synthetic Drugs ◽  
Physiologic Activity ◽  
Pharmacologically Active

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

Sign in / Sign up

Export Citation Format

Share Document