scholarly journals Multicomponent Domino Reaction in the Asymmetric Synthesis of Cyclopentan[c]pyran Core of Iridoid Natural Products

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1308
Author(s):  
Alejandro Manchado ◽  
Victoria Elena Ramos ◽  
David Díez ◽  
Narciso M. Garrido
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Asymmetric Synthesis ◽  
Heteronuclear Nmr ◽  
Domino Reaction ◽  
One Pot ◽  
Pharmaceutical Development ◽  
New Drug ◽  
Anti Inflammatory ◽  
Pharmaceutical Properties

The asymmetric synthesis of a compound with the cyclopentan[c]pyran core of iridoid natural products in four steps and 40% overall yield is reported. Our methodology includes a one-pot tandem domino reaction which provides a trisubstituted cyclopentane with five new completely determined stereocenters, which were determined through 2D homo and heteronuclear NMR and n.O.e. experiments on different compounds specially designed for this purpose, such as a dioxane obtained from a diol. Due to their pharmaceutical properties, including sedative, analgesic, anti-inflammatory, CNS depressor or anti-conceptive effects, this methodology to produce the abovementioned iridoid derivatives, is an interesting strategy in terms of new drug discovery as well as pharmaceutical development.

scholarly journals Synthesis of highly substituted 2-spiropiperidines

2018 ◽  
Vol 16 (36) ◽  
pp. 6663-6674 ◽  
Author(s):  
Samuel D. Griggs ◽  
Nathan Thompson ◽  
Daniel T. Tape ◽  
Marie Fabre ◽  
Paul A. Clarke
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
One Pot ◽  
Natural Products Synthesis

Highly substituted novel 2-spiropiperidines, which are scaffolds suitable for drug discovery or natural products synthesis, were synthesized in a simple one-pot or two-pot procedure.

scholarly journals UsingDrosophilaas a platform for drug discovery from natural products in Parkinson's disease

MedChemComm ◽  
2019 ◽  
Vol 10 (6) ◽  
pp. 867-879 ◽  
Author(s):  
Urmila Maitra ◽  
Lukasz Ciesla
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Natural Products ◽  
Drug Discovery ◽  
Therapeutic Potential ◽  
Natural Extracts ◽  
New Drug ◽  
Screening Platform ◽  
Drug Leads

The review provides an overview of discovery of new drug leads from natural extracts usingDrosophilaas a screening platform to evaluate the therapeutic potential of phytochemicals against Parkinson's disease.

The one pot asymmetric synthesis of 3,3′-pyrrolidonyl spiroxindoles via a regio- and stereoselective domino reaction

2019 ◽  
Vol 17 (35) ◽  
pp. 8140-8148
Author(s):  
Saumen Hajra ◽  
Suhas Shivajirao Bhosale ◽  
Atanu Hazra ◽  
Nikhil Kanaujia
Keyword(s):  
Asymmetric Synthesis ◽  
Domino Reaction ◽  
One Pot ◽  
The One

The asymmetric synthesis of 4-aryl-3,3′-spiropyrrolidonyl oxindoles with excellent stereoselectivity (dr >99 : 1 and an ee up to >99%) was achieved via a domino reaction.

ChemInform Abstract: Asymmetric Synthesis of Tetrahydropyridines via an Organocatalytic One-Pot Multicomponent Michael/Aza-Henry/Cyclization Triple Domino Reaction.

ChemInform ◽  
2015 ◽  
Vol 46 (18) ◽  
pp. no-no
Author(s):  
Marcus Bluemel ◽  
Pankaj Chauhan ◽  
Robert Hahn ◽  
Gerhard Raabe ◽  
Dieter Enders
Keyword(s):  
Asymmetric Synthesis ◽  
Domino Reaction ◽  
One Pot

scholarly journals Are we seeing a resurgence in the use of natural products for new drug discovery?

2019 ◽  
Vol 14 (5) ◽  
pp. 417-420 ◽  
Author(s):  
Feng Li ◽  
Yongli Wang ◽  
Dapeng Li ◽  
Yilun Chen ◽  
Q. Ping Dou
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
New Drug

scholarly journals Step economy in the Stereoselective Synthesis of Functionalized Oxindoles via Organocatalytic Domino/One-pot Reactions

2021 ◽  
Vol 25 ◽  
Author(s):  
Martina Bortolami ◽  
Francesca Leonelli ◽  
Marta Feroci ◽  
Fabrizio Vetica
Keyword(s):  
Natural Products ◽  
Asymmetric Synthesis ◽  
Bioactive Compounds ◽  
Stereoselective Synthesis ◽  
Environmentally Friendly ◽  
Important Class ◽  
One Pot ◽  
Asymmetric Organocatalysis ◽  
Toxic Approach

: Oxindoles are an important class of heterocyclic scaffolds widely present in natural products and bioactive compounds. For this reason, a plethora of methodologies for the stereoselective synthesis of enantioenriched oxindoles has been studied over the years. Among all the reported synthetic strategies, organocatalysis has proven to be a powerful tool for the asymmetric synthesis of this class of compounds being a step- and atom-economical, environmentally friendly, and non-toxic approach. This review will outline the application of asymmetric organocatalysis in the synthesis of chiral oxindole-based structures, relying on domino/one-pot reaction sequences in a step-economical fashion.

Natural Products with tandem Anti-inflammatory, Immunomodulatory and Anti-SARS-CoV/2 effects: A Drug Discovery Perspective against SARS-CoV-2

2021 ◽  
Vol 28 ◽  
Author(s):  
Luana N. O. Leal da Cunha ◽  
Tiago Tizziani ◽  
Gabriella B. Souza ◽  
Monalisa A. Moreira ◽  
José S. S. Neto ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
In Silico ◽  
Biological Activities ◽  
Cysteine Proteases ◽  
Drug Candidate ◽  
Plant Metabolites ◽  
Drug Candidates ◽  
In Silico Studies ◽  
Anti Inflammatory

Background: COVID-19 is still causing victims with long-term health consequences, mass deaths, and collapsing healthcare systems around the world. The disease has no efficient drugs. However, previous studies revealed that SARS-CoV-2 and SARS-CoV have 96% and 86.5% similarities in cysteine proteases (3CLpro) and papain-like protease (PLpro) sequences, respectively. This resemblance could be significant in the search for drug candidates with antiviral effects against SARS-CoV-2. Objective: This paper is a compilation of natural products that inhibit SARS-CoV 3CLpro and PLpro and, concomitantly, reduce inflammation and/or modulate the immune system as a perspective strategy for COVID-19 drug discovery. It also presents in silico studies performed on these selected natural products using SARS-CoV-2 3CLpro and PLpro as targets to propose a list of hit compounds. Method: The plant metabolites were selected in the literature based on their biological activities on SARS-CoV proteins, inflammatory mediators, and immune response. The consensus docking analysis was performed using four different packages. Results: Seventy-nine compounds reported in the literature with inhibitory effects on SARS-CoV proteins were reported as anti-inflammatory agents. Fourteen of them showed in previous studies immunomodulatory effects. Five and six of these compounds showed significant in silico consensus as drug candidates that can inhibit PLpro and 3CLpro, respectively. Our findings corroborated recent results reported on anti-SARS-CoV-2 in the literature. Conclusion: This study revealed that amentoflavone, rubranoside B, savinin, psoralidin, hirsutenone, and papyriflavonol A are good drug candidate for the search of antibiotics against COVID-19.

Origins, Structures, and Bioactivities of Secondary Metabolites from Marine-derived Penicillium Fungi

2021 ◽  
Vol 21 ◽  
Author(s):  
Xiliang Yang ◽  
Jinping Liu ◽  
Jiahui Mei ◽  
Rui Jiang ◽  
Shizheng Tu ◽  
...  
Keyword(s):  
Natural Products ◽  
Secondary Metabolites ◽  
Drug Development ◽  
Valuable Source ◽  
Chemical Structures ◽  
New Drug ◽  
Bioactive Properties ◽  
Potential Applications ◽  
New Drug Development ◽  
Anti Inflammatory

: In recent years, marine-derived Penicillium fungi have received remarkable interest as a valuable source of novel natural products encompassing diverse chemical structures and bioactive properties. Mangroves, sediments, algae, and sponges are the four main sources of marine-derived Penicillium fungi. As of 2014, more than 390 novel natural products have been isolated from the marine-derived Penicillium fungi, mainly including polyketides, alkaloids, terpenoids, and macrolides. Biological investigations have shown that these compounds possess antimicrobial, anti-inflammatory, cytotoxic, and other activities with potential applications in new drug development. To provide an updated catalog of this field, our mini-review summarized the origins, structures, and bioactivities of 188 secondary metabolites from marine-derived Penicillium fungi based on bioactivities classification published from 2015 to 2020.

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