Recent advances in the discovery and design of multicomponent reactions for the generation of small-molecule libraries

Malinakova, Helena C.

doi:10.2147/roc.s65115

Cited by 30 publications

(11 citation statements)

References 44 publications

(72 reference statements)

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“…As regards the synthetic methodologies used in these studies, it is worth noting that multicomponent condensation reactions, a class of benign processes that are characterised by experimental simplicity and low cost, have frequently been used for the synthesis of a variety of hybrids and conjugates [9,93,97,145,164,166,[176][177][178]219,220,232,237], and that such processes [250][251][252][253] as well as several other condensation reactions have often been preferentially carried out using microwave (MW)-promoted reactions instead of conventional heating sources [254][255][256][257][258]. In fact, as often highlighted by the published data, the advantages of microwave-promoted reactions [93,144,166,177,219,232] include significant shorter reaction times, higher yields, and product purity when compared to conventional thermal methods.…”

Section: Discussionmentioning

confidence: 99%

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

Rossi

Ciofalo

2020

Molecules

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The rapid growth of serious infections caused by antibiotic resistant bacteria, especially the nosocomial ESKAPE pathogens, has been acknowledged by Governments and scientists and is one of the world’s major health problems. Various strategies have been and are currently investigated and developed to reduce and/or delay the bacterial resistance. One of these strategies regards the design and development of antimicrobial hybrids and conjugates. This unprecedented critical review, in which our continuing interest in the synthesis and evaluation of the bioactivity of imidazole derivatives is testified, aims to summarise and comment on the results obtained from the end of the 1900s until February 2020 in studies conducted by numerous international research groups on the synthesis and evaluation of the antibacterial properties of imidazole-based molecular hybrids and conjugates in which the pharmacophoric constituents of these compounds are directly covalently linked or connected through a linker or spacer. In this review, significant attention was paid to summarise the strategies used to overcome the antibiotic resistance of pathogens whose infections are difficult to treat with conventional antibiotics. However, it does not include literature data on the synthesis and evaluation of the bioactivity of hybrids and conjugates in which an imidazole moiety is fused with a carbo- or heterocyclic subunit.

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Section: Discussionmentioning

confidence: 99%

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

Rossi

Ciofalo

2020

Molecules

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“…Multicomponent reactions (MCRs) are considered to be very important and powerful reactions in combinatorial and medicinal chemistry [57] because of the benefits they offer in terms of the synthesis of diverse structures that will lead to an increase in the economy of organic synthesis [58,59] by shortening the time span [60].…”

Section: Chemistrymentioning

confidence: 99%

One-Pot Multicomponent Synthesis and Bioevaluation of Tetrahydroquinoline Derivatives as Potential Antioxidants, α-Amylase Enzyme Inhibitors, Anti-Cancerous and Anti-Inflammatory Agents

et al. 2020

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Mankind has always suffered from multiple diseases. Therefore, there has been a rigorous need in the field of medicinal chemistry for the design and discovery of new and potent molecular entities. In this work, thirteen tetrahydroquinoline derivatives were synthesized and evaluated biologically for their antioxidant, α-amylase enzyme inhibitory, anti-proliferative and anti-inflammatory activities. SF8 showed the lowest IC50 of 29.19 ± 0.25 µg/mL by scavenging DPPH free radicals. SF5 showed significant antioxidant activity in total antioxidant capacity (TAC) and total reducing power (TRP) assays. SF5 and SF9 showed the maximum inhibition of α-amylase enzyme i.e., 97.47% and 89.93%, respectively, at 200 µg/mL concentration. Five compounds were shortlisted to determine their anti-proliferative potential against Hep-2C cells. The study was conducted for 24, 48 and 72 h. SF8 showed significant results, having an IC50 value of 11.9 ± 1.04 µM at 72 h when compared with standard cisplatin (IC50 value of 14.6 ± 1.01 µM). An in vitro nitric oxide (NO) assay was performed to select compounds for in vivo anti-inflammatory activity evaluation. SF13 scavenged the NO level to a maximum of 85% at 50 µM concentration, followed by SF1 and SF2. Based on the NO scavenging assay results, in vivo anti-inflammatory studies were also performed and the results showed significant activity compared to the standard, acetylsalicylic acid (ASA).

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“…This method proved to be of considerable utility to researchers to obtain desired complex heterocyclic frameworks by condensation of more than two reactants in a single operational step. [41][42][43][44][45][46][47][48] Herein, in continuation of studies towards the synthesis of heterocyclic scaffolds via multicomponent reactions, [49][50][51][52] and because the 6-aminouracil is frequently used as a starting material in synthesizing these compounds. This review is devoted to recent applications of 6-aminouracil and its derivatives in synthesizing diverse heterocyclic compounds based on MCRs from 2015 to 2020.…”

Section: Introductionmentioning

confidence: 99%

Recent applications of aminouracil in multicomponent reactions

Javahershenas¹

2021

Arkivoc

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6-Aminouracil and its derivatives are versatile heterocyclic compounds and are frequently employed to synthesize a wide array of fused uracils annulated with other heterocyclic rings which can serve to address biological and pharmacological targets. Multicomponent reactions (MCRs) are important in the synthesis of natural products and pharmaceuticals by forming heterocyclic molecular frameworks with generally high atom-economy in a single reaction step. This review embraces various modern synthetic strategies, summarizing recent research developments providing fused 6-aminouracil derivatives and to highlight the progress based on MCRs between 2015 and 2020.

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Recent advances in the discovery and design of multicomponent reactions for the generation of small-molecule libraries

Cited by 30 publications

References 44 publications

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

One-Pot Multicomponent Synthesis and Bioevaluation of Tetrahydroquinoline Derivatives as Potential Antioxidants, α-Amylase Enzyme Inhibitors, Anti-Cancerous and Anti-Inflammatory Agents

Recent applications of aminouracil in multicomponent reactions

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