scholarly journals Synthesis of Biologically Active Molecules through Multicomponent Reactions

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 505 ◽  
Author(s):  
Daniel Insuasty ◽  
Juan Castillo ◽  
Diana Becerra ◽  
Hugo Rojas ◽  
Rodrigo Abonia
Keyword(s):  
Multicomponent Reaction ◽  
Biological Property ◽  
Multicomponent Reactions ◽  
Organic Molecules ◽  
Biological Activities ◽  
Biologically Active ◽  
Vast Number ◽  
Key Points ◽  
Reported Data ◽  
Synthetic Approaches

Focusing on the literature progress since 2002, the present review explores the highly significant role that multicomponent reactions (MCRs) have played as a very important tool for expedite synthesis of a vast number of organic molecules, but also, highlights the fact that many of such molecules are biologically active or at least have been submitted to any biological screen. The selected papers covered in this review must meet two mandatory requirements: (1) the reported products should be obtained via a multicomponent reaction; (2) the reported products should be biologically actives or at least tested for any biological property. Given the diversity of synthetic approaches utilized in MCRs, the highly diverse nature of the biological activities evaluated for the synthesized compounds, and considering their huge structural variability, much of the reported data are organized into concise schemes and tables to facilitate comparison, and to underscore the key points of this review.

Synthetic approaches toward diversely substituted 1,2,2-triarylethanones

2021 ◽  
Vol 25 ◽  
Author(s):  
Rodrigo Abonia ◽  
Oscar Montoya
Keyword(s):  
Carbonyl Compounds ◽  
Bond Activation ◽  
Building Blocks ◽  
Biologically Active ◽  
Carbon Carbon Bond ◽  
Key Points ◽  
Carbon Carbon Bonds ◽  
Reported Data ◽  
Synthetic Approaches ◽  
Free Metal

: Carbon–carbon bond formation is the essence of organic synthesis, and for that, many strategies have been developed to accomplish this goal. Several of these strategies are conducted to form diverse structures bearing the α,α-diarylcarbonyl motif, in form of 1,2,2-triarylethanones, which are unities present in a number of natural products and biologically active compounds.These privileged carbonyl compounds have been used as building blocks or intermediates for the synthesis of dibenzo[a,c]phenanthridines, analogues of biologically active benzo[c]phenanthridine alkaloids, as well as, a useful synthon for Droloxifene and remarkably for Tamoxifen, the most widely used drug for the treatment of breast cancer. Focusing on the literature progress since 2000 to 2020 and considering the synthetic and biologically value of the aforementioned carbonyl compounds, the present review explores the diverse metal-free, metal-mediated, C–H bond activation, α-monoarylation, α,α-diarylation, umpolung processes, N-heterocyclic carbene (NHC), deoxygenation, among others,synthetic approaches directed to the synthesis of 1,2,2-triarylethanone derivatives. Moreover, several of their mechanistic proposals are also briefly discussed in this review. In view that most of these strategies are accompanied of carbon–carbon bonds formation through ketone-based α-arylation processes,the reported data are organized into concise Tables/Schemes to facilitate comparison, and to underscore the key points of this review.

Halogenated Flavones and Isoflavones: A State-of-Art on their Synthesis

2020 ◽  
Vol 17 (6) ◽  
pp. 415-425
Author(s):  
Ricardo Santos ◽  
Diana Pinto ◽  
Clara Magalhães ◽  
Artur Silva
Keyword(s):  
Biological Activities ◽  
New Drugs ◽  
Reaction Conditions ◽  
Balanced Diet ◽  
Wide Range ◽  
The Everyday ◽  
Synthetic Routes ◽  
Scopus Database ◽  
Reported Data ◽  
Synthetic Approaches

Background: Flavonoid is a family of compounds present in the everyday consumption plants and fruits, contributing to a balanced diet and beneficial health effects. Being a scaffold for new drugs and presenting a wide range of applicability in the treatment of illnesses give them also an impact in medicine. Among the several types of flavonoids, flavone and isoflavone derivatives can be highlighted due to their prevalence in nature and biological activities already established. The standard synthetic route to obtain both halogenated flavones and isoflavones is through the use of already halogenated starting materials. Halogenation of the flavone and isoflavone core is less common because it is more complicated and involves some selectivity issues. Objective: Considering the importance of these flavonoids, we aim to present the main and more recent synthetic approaches towards their halogenation. Methods: The most prominent methodologies for the synthesis of halogenated flavones and isoflavones were reviewed. A careful survey of the reported data, using mainly the Scopus database and halogenation, flavones and isoflavones as keywords, was conducted. Results: Herein, a review is provided on the latest and more efficient halogenation protocols of flavones and isoflavones. Selective halogenation and the greener methodologies, including enzymatic and microbial halogenations, were reported. Nevertheless, some interesting protocols that allowed the synthesis of halogenated flavone and isoflavone derivatives in specific positions using halogenated reagents are also summarized. Conclusion: Halogenated flavones and isoflavones have risen as noticeable structures; however, most of the time, the synthetic procedures involve toxic reagents and harsh reaction conditions. Therefore, the development of new synthetic routes with low environmental impact is desirable.

An Insight into Synthetic Strategies for Schiff Base Derivatives with Diverse Biological Activities

2020 ◽  
Vol 17 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A. Chawla ◽  
Md. Jawaid Akhtar ◽  
Bhupinder Kumar
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Biological Activities ◽  
Biologically Active ◽  
Biological Processes ◽  
Schiff Base Derivatives ◽  
Active Moiety ◽  
Comprehensive Knowledge ◽  
Key Points ◽  
Insight Into

Abstract:: Schiff base or imine or azomethine is one of the most important organic compounds that has been reported to play a significant role in various biological processes. The group is a part of natural or non-natural compounds and is involved as important precursors as diversified agents and as intermediates for the synthesis of biologically active agents. The review outlines the detailed design strategy, synthesis and structure-activity relationship studies of different Schiff bases for various biological activities. We have tried to outline the key points of various researchers with respect to biological activities. The results of different studies demonstrate Schiff bases as a linker in many synthetic compounds displaying a broad range of activities. We believe that the present review will provide comprehensive knowledge about medicinal importance of Schiff bases and serve as important literature in designing the synthesis of novel molecules containing Schiff base as pharmacophore or biologically active moiety.

A Mini Review on Synthesis of Pyrazinoindole: Recent Progress and Perspectives

2020 ◽  
Vol 17 ◽  
Author(s):  
Aarushi Singh ◽  
Samarpita Mahapatra ◽  
Shubham Sewariya ◽  
Nidhi Singh ◽  
Snigdha Singh ◽  
...  
Keyword(s):  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring Structure ◽  
Biologically Active ◽  
Comprehensive Overview ◽  
Protein Kinase C Inhibitors ◽  
Therapeutic Uses ◽  
Recent Developments ◽  
Pharmacologically Active ◽  
Synthetic Approaches

: The diverse library of biologically active organic compounds is composed majorly of heterocyclic compounds. Nature provides us with a variety of pharmacologically active compounds consisting of N-heterocycle motif such as Noscapine (anti-cancer), Morphine (analgesic), Chelerythrine (antibacterial), etc. which are the elementary structural units of marketed drugs in the present era. One of such “N-heterocyclic” promising building block which has gained attention of chemists is Pyrazinoindoles and the inflating interest in this moiety is a result of the three-fused heterocyclic ring structure subsuming an indolic nucleus in it. Fused-polycyclic structural core is necessary to synthesize for potential multi-functional drugs which is evident from indole (an example of fused five and six-membered ring structure) being an exemplary, established privileged template in medicinal chemistry. In the literature, Pyrazino-fused indoles have been found documented regarding their biological activities and therapeutic uses particularly as antifungal, antibacterial, serotonergic receptor inhibitor, central nervous system depressants, anticonvulsants, antihistaminic, protein kinase C inhibitors, antidepressants and so on. Although various synthesis strategies are available in the literature yet the medical relevance of the Pyrazinoindoles demands the development of versatile and simple novel methodologies. This review features comprehensive overview of the recent developments in synthetic approaches and therapeutic applications of Pyrazinoindoles based scaffolds.

One-pot Synthesis of Pyrano[2,3-c]pyrazole Derivatives via Multicomponent Reactions (MCRs) and their Applications in Medicinal Chemistry

2021 ◽  
Vol 19 ◽  
Author(s):  
Swapan Kumar Biswas ◽  
Debasis Das
Keyword(s):  
Multicomponent Reactions ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Pyrazole Derivatives ◽  
One Pot ◽  
Discovery Research ◽  
Drug Discovery Research ◽  
Biological Interest ◽  
Derivatives Of

Background: Many pyrano[2,3-c]pyrazole derivatives display diverse biological activities and some of them are known as anticancer, analgesic, anticonvulsant, antimicrobial, anti-inflammatory, and anti-malarial agents. In recent years, easy convergent, multicomponent reactions (MCRs) have been adopted to make highly functionalizedpyrano[2,3-c]pyrazole derivatives of biological interest. The synthesis of 1,4-dihydropyrano[2,3-c]pyrazole (1,4-DHPP, 2), 2,4-dihydropyrano[2,3-c]pyrazole (2,4-DHPP, 3), 4-hydroxypyrano[2,3-c]pyrazole (4-HPP, 4) derivatives, 1,4,4-substitied pyranopyrazole (SPP, 5) were reported via two-, three-, four- and five-component reactions (MCRs). Methods: This review article compiles the preparation of pyrano[2,3-c]pyrazole derivatives, and it highlights the applications of various pyrano[2,3-c]pyrazole derivatives in medicinal chemistry. Results: Varieties of pyrano[2,3-c]pyrazole derivatives were achieved via “One-pot” multicomponent reactions (MCRs). Different reaction conditions in the presence of a catalyst or without catalysts were adapted to prepare the pyrano[2,3-c]pyrazole derivatives. Conclusion: Biologically active pyrano[2,3-c]pyrazole derivatives were prepared and used in drug discovery research.

Recent Advances in the Exploitation of Kojic Acid in Multicomponent Reactions

2020 ◽  
Vol 24 (14) ◽  
pp. 1643-1662
Author(s):  
Ankita Chaudhary
Keyword(s):  
Multicomponent Reactions ◽  
Kojic Acid ◽  
Biological Activities ◽  
Biologically Active ◽  
Atom Economy ◽  
One Pot ◽  
Biologically Relevant ◽  
Modern Drug ◽  
Wide Range ◽  
Active Precursor

Kojic acid, one of the most widespread 3-hydroxypyran-4-one derivatives, displays a wide range of biological activities and found application in food as well as cosmetics industry. The synthesis of kojic acid derivatives has provoked great interest as an easily available and biologically active precursor among organic and medicinal researchers. Multicomponent reactions, involving three or more reactants in one-pot thereby resulting in a structure with functional diversity are efficient methods for the promotion of green chemistry in the context of modern drug discovery. They offer several advantages over conventional stepwise protocols like simplicity, efficiency, selectivity, convergence and atom economy. This review aims to highlight the versatility of kojic acid as an important synthon in multicomponent reactions for the construction of various biologically relevant compounds such as pyrano[3,2‐ b]chromenediones, pyrano[3,2-b]pyrans, pyrano[2′,3′:5,6]pyrano[2,3‑b]pyridines, spiro[indoline-3,4’-pyrano[3, 2-b]pyrans, 2-substituted kojic acid conjugates, etc.

Recent Progress in the Synthesis of Pyrimidine Heterocycles: A Review

2020 ◽  
Vol 24 (10) ◽  
pp. 1055-1096
Author(s):  
Pradip Kumar Maji
Keyword(s):  
Broad Spectrum ◽  
Recent Progress ◽  
Biological Activities ◽  
Building Blocks ◽  
Heterocyclic Ring ◽  
Antibacterial Activities ◽  
Review Article ◽  
Biologically Active ◽  
Synthetic Strategy ◽  
Synthetic Approaches

Pyrimidine heterocycles are proven to be biologically active heterocycles, found in many biological systems, displaying a broad spectrum of biological activities including anticancer, anxiolytic, antioxidant, antiviral, antifungal, anticonvulsant, antidepressant and antibacterial activities. Recently, various synthetic approaches, synthetic strategy, the variation of substrates and study devoted towards the evaluation of biological activities for the pyrimidine heterocycles have been reported in the literature. This review article describes the synthesis of various biologically interesting pyrimidine heterocyclic ring systems using various nitrogen building blocks.

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.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

Reactivity of Barbituric, Thiobarbituric Acids and Their Related Analogues: Synthesis of Substituted and Heterocycles-based Pyrimidines

2020 ◽  
Vol 24 (14) ◽  
pp. 1610-1642 ◽  
Author(s):  
Ahmed El-Mekabaty ◽  
Hassan A. Etman ◽  
Ahmed Mosbah ◽  
Ahmed A. Fadda
Keyword(s):  
Xanthine Oxidase ◽  
Multicomponent Reactions ◽  
Biological Activities ◽  
Present Review ◽  
Urease Inhibitors ◽  
Effective Catalyst ◽  
Inhibitory Activities ◽  
Catalyst Reusability ◽  
High Yields ◽  
Nano Catalysts

Barbituric, thiobarbituric acids and their related analogs are reactive synthons for the synthesis of drugs and biologically, and pharmaceutically active pyrimidines. The present review aimed to summarize the recent advances in the synthesis of different alkylsubstituted, fused cycles, spiro-, and binary heterocycles incorporated pyrimidine skeleton based on barbituric derivatives. In this sequence, the eco-friendly techniques under catalytic conditions were used for the diverse types of multicomponent reactions under different conditions for the synthesis of various types of heterocycles. Nano-catalysts are efficient for the synthesis of these compounds in high yields and effective catalyst reusability. The compounds are potent antibacterial, cytotoxic, xanthine oxidase inhibitory activities, and attend as urease inhibitors. The projected mechanisms for the synthesis of pyranopyrimidines, benzochromenopyrimidines, chromeno-pyranopyrimidines, spiroxyindoles, oxospiro-tricyclic furopyrimidines, pyrimidine-based monoand bicyclic pyridines were discussed. The potent and diverse biological activities for instance, antioxidant, antibacterial, cytotoxic, and xanthine oxidase inhibitory activities, as well as urease inhibitors, are specified.

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