Recent Synthetic Methodologies for Chalcone Synthesis (2013-2018)

Ngaini, Zainab

doi:10.2174/2213337206666190306155140

Cited by 46 publications

(28 citation statements)

References 147 publications

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“…The synthesis of epoxy chalcone via two-pot methodology is the most commonly reported. The preparation has been performed via the formation of α,β-enones [64] prior to the cyclization and epoxidation reaction (Scheme 2) [65][66][67][68][69][70][71][72].…”

Section: Two-pot Routementioning

confidence: 99%

One Pot and Two Pot Synthetic Strategies and Biological Applications of Epoxy-Chalcones

Farooq

Ngaini

2020

Chemistry Africa

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Epoxy chalcone is a heterocyclic molecule and an important precursor for the synthesis of biologically active compounds. This mini-review is elucidating the synthetic strategies of chalcone epoxide via one pot and two pot routes including nature of reactants, nature of catalyst and variety of catalyst to improve yield of desired product, biological applications and advantages and drawbacks of these synthetic strategies. One pot route has wide variety of reactants and efficient one is the condensation of aldehyde and ketone. However, two pot route is consisted of chalcone synthesis preceding to epoxy chalcone. The synthetic routes for the preparation of epoxy chalcone and the usage as a precursor for the synthesis of various organic molecules with biological application is comprehensively discussed. This review is outstanding in organic chemistry and pharmaceutical industries to produce new molecules with various applications. Graphic AbstractO O

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Section: Two-pot Routementioning

confidence: 99%

One Pot and Two Pot Synthetic Strategies and Biological Applications of Epoxy-Chalcones

Farooq

Ngaini

2020

Chemistry Africa

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“…The flavonoid-type compounds named chalcones and flavanones are natural isomeric compounds which exhibit a broad range of patented therapeutic applications [63]. Since they are chemically very labile, chalcones and flavanones are also excellent scaffolds to medicinal chemistry and development of new drugs [64][65][66]. In this context, the optimization of the aldol condensation synthesis route by using unexplored bases to prepare hydroxylated and methoxylated chalcones and flavanones proposed by Rosa et al [67] is well come.…”

Section: Contributionsmentioning

confidence: 99%

Natural Compounds: A Dynamic Field of Applications

Seca

Moujir

2020

Applied Sciences

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Nature represents an amazing source of inspiration since it produces a great diversity of natural compounds selected by evolution, which exhibit multiple biological activities and applications. A large and very active research field is dedicated to identifying biosynthesized compounds, to improve/develop new methodologies to produce/reuse natural compounds and to assess their potential for pharmaceutical, cosmetic and food industries, among others, and also to understand their mechanism of action. Here, the main results presented in each work are highlighted. The applications suggested are mostly related to pharmacological uses and involve mainly pure natural compounds and essential oils. These works are significant contributions and reinforce the dynamic field of natural products applications.

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“…Chalcone is a biologically active molecule derived from natural products. Chalcone and their derivatives can be easily prepared via Claisen‐Schmidt condensation 1 . It has a distinctive open chain flavonoid with two aromatic rings and three carbon atoms.…”

Section: Introductionmentioning

confidence: 99%

Microwave‐assisted Synthesis and Molecular Docking Study of Heteroaromatic Chalcone Derivatives as Potential Antibacterial Agents

Farooq

Ngaini

Mortadza

2020

Bulletin Korean Chem Soc

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In this study, a series of chalcone derivatives (1a-c) were synthesized via Claisen-Schmidt condensation, followed by aza-Michael addition to form pyrazoline derivatives (2a-c and 3a-c). The reaction was performed via microwave radiation to give excellent yields (77-93%) in 1-3.5 min. Microwave-assisted reaction of Fischer esterification of pyrazolines (2a-c and 3a-c) afforded heteroaromatic pyrazoline esters (4a-c) in high yield (83-96% in <2 min) compared to conventional reflux (55-79% in 30 min). Compounds 1a-c and 3a-c demonstrated excellent antibacterial activity against Staphylococcus aureus via disc diffusion assay with inhibition zone with 13 and 19 mm compared to a standard drug, ampicillin (11 mm). Structure activity relationship of 1b and 3b were visualized via molecular docking interaction against 4pql protein of S. aureus with binding free energy −7.0 and −8.0 kcal/mol, respectively. This study is significant in drug discovery process particularly for pharmaceutical industries.

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Recent Synthetic Methodologies for Chalcone Synthesis (2013-2018)

Cited by 46 publications

References 147 publications

One Pot and Two Pot Synthetic Strategies and Biological Applications of Epoxy-Chalcones

One Pot and Two Pot Synthetic Strategies and Biological Applications of Epoxy-Chalcones

Natural Compounds: A Dynamic Field of Applications

Microwave‐assisted Synthesis and Molecular Docking Study of Heteroaromatic Chalcone Derivatives as Potential Antibacterial Agents

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