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Article ; Online: Expanding Chemical Frontiers: Approaches for Generating Diverse and Bioactive Natural Product-Like Compounds Libraries from Extracts.

Beato, Aurélien / Haudecoeur, Romain / Boucherle, Benjamin / Peuchmaur, Marine

Chemistry (Weinheim an der Bergstrasse, Germany)

2024 , Page(s) e202304166

Abstract: The realms of natural products and synthetic compounds exhibit distinct chemical spaces that not only differ but also complement each other. While the convergence of these two domains has been explored through semisynthesis and conventional ... ...

Abstract	The realms of natural products and synthetic compounds exhibit distinct chemical spaces that not only differ but also complement each other. While the convergence of these two domains has been explored through semisynthesis and conventional pharmacomodulation endeavours applied to natural frameworks, a recent and innovative approach has emerged that involves the combinatorial generation of libraries of 'natural product-like compounds' (NPLCs) through the direct synthetic derivatization of natural extracts. This has led to the production of numerous NPLCs that incorporate structural elements from both their natural (multiple saturated rings, oxygen content, chiral centres) and synthetic (aromatic rings, nitrogen and halogen content, drug-like properties) precursors. Through careful selection of extracts and reagents, specific bioactivities have been achieved, and this strategy has been deployed in various ways, showing great promise without reaching its full potential to date. This review seeks to provide an overview of reported examples involving the chemical engineering of extracts, showcasing a spectrum of natural product alterations spanning from simple substitutions to complete scaffold remodelling. It also includes an analysis of the accomplishments, perspectives and technical challenges within this field.
Language	English
Publishing date	2024-02-19
Publishing country	Germany
Document type	Journal Article ; Review
ZDB-ID	1478547-X
ISSN	1521-3765 ; 0947-6539
ISSN (online)	1521-3765
ISSN	0947-6539
DOI	10.1002/chem.202304166
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.

Beato, Aurélien / Gori, Anthonin / Boucherle, Benjamin / Peuchmaur, Marine / Haudecoeur, Romain

Journal of medicinal chemistry

2021 Volume 64, Issue 3, Page(s) 1392–1422

Abstract: The natural β-carboline alkaloids display similarities with neurotransmitters that can be favorably exploited to design bioactive and bioavailable drugs for Alzheimer's disease (AD) therapy. Several AD targets are currently and intensively being ... ...

Abstract	The natural β-carboline alkaloids display similarities with neurotransmitters that can be favorably exploited to design bioactive and bioavailable drugs for Alzheimer's disease (AD) therapy. Several AD targets are currently and intensively being investigated, divided in different hypotheses: mainly the cholinergic, the amyloid β (Aβ), and the Tau hypotheses. To date, only symptomatic treatments are available involving acetylcholinesterase and NMDA inhibitors. On the basis of plethoric single-target structure-activity relationship studies, the β-carboline scaffold was identified as a powerful tool for fostering activity and molecular interactions with a wide range of AD-related targets. This knowledge can undoubtedly be used to design multitarget-directed ligands, a highly relevant strategy preferred in the context of multifactorial pathology with intricate etiology such as AD. In this review, we first individually discuss the AD targets of the β-carbolines, and then we focus on the multitarget strategies dedicated to the deliberate design of new efficient scaffolds.
MeSH term(s)	Alzheimer Disease/drug therapy ; Animals ; Carbolines/chemistry ; Drug Design ; Humans ; Neurotransmitter Agents/chemistry ; Structure-Activity Relationship
Chemical Substances	Carbolines ; Neurotransmitter Agents
Language	English
Publishing date	2021-02-02
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.0c01887
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Article: Epstein-Barr Virus Encephalitis: A Review of Case Reports from the Last 25 Years.

Peuchmaur, Marine / Voisin, Joris / Vaillant, Mathieu / Truffot, Aurélie / Lupo, Julien / Morand, Patrice / Le Maréchal, Marion / Germi, Raphaele

Microorganisms

2023 Volume 11, Issue 12

Abstract: Although uncommon, Epstein-Barr virus-related neurological disorders represent the seventh most frequent cause of infectious encephalitis in adults. The limited number of publications on EBV encephalitis mainly document isolated clinical cases. This ... ...

Abstract	Although uncommon, Epstein-Barr virus-related neurological disorders represent the seventh most frequent cause of infectious encephalitis in adults. The limited number of publications on EBV encephalitis mainly document isolated clinical cases. This study aimed to summarize published data on EBV encephalitis. A systematic literature search identified 97 EBV encephalitis cases. In the selected cases, EBV-related neurological disorders manifested as lymphocytic pleocytosis in the cerebrospinal fluid (CSF) with moderate hyperproteinorachia. The EBV PCR test was positive in 87% of the CSF samples, with wide-ranging viral loads. When encephalitis occurred in the context of past EBV infections, all of the EBV PCR tests on CSF samples were positive. On the contrary, negative EBV PCR tests on CSF samples occurred only in the context of primary infections. EBV PCR was rarely carried out on blood samples, contributing minimally to the diagnosis. For the treatment of EBV encephalitis, Aciclovir was used alone in 29% of cases, and in association with other drugs in 40% of cases. Ganciclovir (30%), corticoids (52%), and immunoglobulins (15%) were mainly used in association with other drugs. Cerebral imaging was abnormal in 69% of cases, mostly in the cerebellum and basal ganglia. This work highlights that the EBV PCR test on CSF samples is currently the main laboratory diagnostic test to diagnose EBV encephalitis. This diagnostic test is useful; however, it is imperfect. New complementary diagnostic tools, approved treatments, and standardized practices could improve patient management.
Language	English
Publishing date	2023-11-21
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2720891-6
ISSN	2076-2607
ISSN	2076-2607
DOI	10.3390/microorganisms11122825
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Article ; Online: Development of an innovative maceration technique to optimize extraction and phase partition of natural products.

Gori, Anthonin / Boucherle, Benjamin / Rey, Aurélien / Rome, Maxime / Fuzzati, Nicola / Peuchmaur, Marine

Fitoterapia

2020 Volume 148, Page(s) 104798

Abstract: The active component extraction from plants is the first crucial step in natural product research. For non-targeted extraction with an objective to isolate and characterize as many compounds as possible, the most classical technique, and the simplest to ... ...

Abstract	The active component extraction from plants is the first crucial step in natural product research. For non-targeted extraction with an objective to isolate and characterize as many compounds as possible, the most classical technique, and the simplest to implement, is the Soxhlet extraction; however, it does not allow retrieving all the compounds from the plant (when it does not additionally cause artifacts during long heating process). The second most used technique is the extraction by successive macerations using solvents of increasing polarity. While this method is frequently used, few studies are available to rationalize and optimize it. Furthermore, this extraction technique requires some enhancement mainly for efficiency, environmental and time constraint reasons. Here, we present an innovative method of successive macerations using a mixture of solvents with the aim of simultaneously improving the yield, the partition of the compounds between the different phases and reducing the volume of extraction solvents. Triphasic systems were prepared by mixing five solvents (n-heptane, ethyl acetate, acetonitrile, butan-1-ol, water) in various proportions. To validate this method, the most efficient triphasic system was subsequently used to perform three successive macerations with a polarity gradient on a model plant before being extended to several alpine plants. Our results showed an overall good yield compared to conventional maceration techniques, while improving phase partition and reducing extraction time and volume of solvents.
MeSH term(s)	Biological Products/chemistry ; Biological Products/isolation & purification ; Chemical Fractionation/methods ; Phytochemicals/chemistry ; Phytochemicals/isolation & purification ; Solvents
Chemical Substances	Biological Products ; Phytochemicals ; Solvents
Language	English
Publishing date	2020-12-08
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	412385-2
ISSN	1873-6971 ; 0367-326X
ISSN (online)	1873-6971
ISSN	0367-326X
DOI	10.1016/j.fitote.2020.104798
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Article: Investigation of Chemical Composition and Biological Activities of

Gori, Anthonin / Boucherle, Benjamin / Rey, Aurélien / Rome, Maxime / Barette, Caroline / Soleilhac, Emmanuelle / Philouze, Christian / Fauvarque, Marie-Odile / Fuzzati, Nicola / Peuchmaur, Marine

Metabolites

2023 Volume 13, Issue 1

Abstract: Despite several studies on ... ...

Abstract	Despite several studies on the
Language	English
Publishing date	2023-01-14
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2662251-8
ISSN	2218-1989
ISSN	2218-1989
DOI	10.3390/metabo13010128
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Article ; Online: Aurones and derivatives as promising New Delhi metallo-β-lactamase (NDM-1) inhibitors.

Caburet, Jérémy / Verdirosa, Federica / Moretti, Matis / Roulier, Brayan / Simoncelli, Giorgia / Haudecoeur, Romain / Ghazi, Somayeh / Jamet, Hélène / Docquier, Jean-Denis / Boucherle, Benjamin / Peuchmaur, Marine

Bioorganic & medicinal chemistry

2023 Volume 97, Page(s) 117559

Abstract: Bacterial resistance is undoubtedly one of the main public health concerns especially with the emergence of metallo-β-lactamases (MBLs) able to hydrolytically inactivate β-lactam antibiotics. Currently, there are no inhibitors of MBLs in clinical use to ... ...

Abstract	Bacterial resistance is undoubtedly one of the main public health concerns especially with the emergence of metallo-β-lactamases (MBLs) able to hydrolytically inactivate β-lactam antibiotics. Currently, there are no inhibitors of MBLs in clinical use to rescue antibiotic action and the New Delhi metallo-β-lactamase-1 (NDM-1) is still considered as one of the most relevant targets for inhibitor development. Following a fragment-based strategy to find new NDM-1 inhibitors, we identified aurone as a promising scaffold. A series of 60 derivatives were then evaluated and two of them were identified as promising inhibitors with K
MeSH term(s)	Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/chemistry ; Benzofurans ; beta-Lactamase Inhibitors/pharmacology ; beta-Lactamase Inhibitors/chemistry ; beta-Lactamases/chemistry ; Microbial Sensitivity Tests
Chemical Substances	Anti-Bacterial Agents ; aurone ; Benzofurans ; beta-Lactamase Inhibitors ; beta-lactamase NDM-1 (EC 3.5.2.6) ; beta-Lactamases (EC 3.5.2.6)
Language	English
Publishing date	2023-12-12
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1161284-8
ISSN	1464-3391 ; 0968-0896
ISSN (online)	1464-3391
ISSN	0968-0896
DOI	10.1016/j.bmc.2023.117559
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Article ; Online: Occurrences, biosynthesis and properties of aurones as high-end evolutionary products.

Boucherle, Benjamin / Peuchmaur, Marine / Boumendjel, Ahcène / Haudecoeur, Romain

Phytochemistry

2017 Volume 142, Page(s) 92–111

Abstract: Recent years have witnessed a considerable renewed interest for the uncommon flavonoid class of aurones. The characterization of two major biosynthetic machineries involved in their biosynthesis in flowers has encouraged the revival of phytochemical ... ...

Abstract	Recent years have witnessed a considerable renewed interest for the uncommon flavonoid class of aurones. The characterization of two major biosynthetic machineries involved in their biosynthesis in flowers has encouraged the revival of phytochemical studies and identification of original structures, a process started almost seventy-five years ago. This review draws up an exhaustive map of natural occurrences of aurones their biosynthetic pathways and roles, with the aim to link their original structural properties among flavonoids to their place in evolution and the selective advantages they bring to some of the most advanced taxa in the plant kingdom.
MeSH term(s)	Anacardiaceae/chemistry ; Benzofurans/chemistry ; Biological Products/chemistry ; Fabaceae/chemistry ; Flavonoids/chemistry ; Flowers/chemistry ; Molecular Structure ; Rhamnaceae/chemistry
Chemical Substances	Benzofurans ; Biological Products ; Flavonoids ; aurone
Language	English
Publishing date	2017-10
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	208884-8
ISSN	1873-3700 ; 0031-9422
ISSN (online)	1873-3700
ISSN	0031-9422
DOI	10.1016/j.phytochem.2017.06.017
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Article ; Online: Exploring the structure-activity relationship of benzylidene-2,3-dihydro-1H-inden-1-one compared to benzofuran-3(2H)-one derivatives as inhibitors of tau amyloid fibers.

Boukherrouba, Emeline / Larosa, Camille / Nguyen, Kim-Anh / Caburet, Jérémy / Lunven, Laurent / Bonnet, Hugues / Fortuné, Antoine / Boumendjel, Ahcène / Boucherle, Benjamin / Chierici, Sabine / Peuchmaur, Marine

European journal of medicinal chemistry

2022 Volume 231, Page(s) 114139

Abstract: Tauopathies, such as Alzheimer's disease, have been the subject of several hypotheses regarding the way to treat them. Hyperphosphorylation of tau protein leading to its aggregation is widely recognized as a key step in the development of these diseases ... ...

Abstract	Tauopathies, such as Alzheimer's disease, have been the subject of several hypotheses regarding the way to treat them. Hyperphosphorylation of tau protein leading to its aggregation is widely recognized as a key step in the development of these diseases resulting in neuronal dysfunction. The AcPHF6 model of tau that includes the shorter critical fragment involved in the protein aggregation was used in vitro to identify new potential inhibitors. Following a previous study on aurone derivatives, we herein compare this polyphenol family to a very close one, the benzylidene-2,3-dihydro-1H-inden-1-one (also named indanone). The structure activity relationship studies bring to light the importance of the hydroxylation pattern in both series: the more hydroxylated, the more active. In addition, the three-dimensional shape of the molecules is involved in their interaction mode with their target, thus defining their role either as inhibitors of fiber elongation or as fiber-binding molecules. Indanone 13a was identified as a promising inhibitor: its activity was confirmed by circular dichroism and atomic force microscopy studies.
MeSH term(s)	Alzheimer Disease ; Benzofurans/chemistry ; Benzofurans/pharmacology ; Humans ; Protein Aggregates ; Structure-Activity Relationship ; tau Proteins/metabolism
Chemical Substances	Benzofurans ; Protein Aggregates ; tau Proteins
Language	English
Publishing date	2022-01-21
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2022.114139
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Article ; Online: A fragment-based drug discovery strategy applied to the identification of NDM-1 β-lactamase inhibitors.

Caburet, Jérémy / Boucherle, Benjamin / Bourdillon, Sofiane / Simoncelli, Giorgia / Verdirosa, Federica / Docquier, Jean-Denis / Moreau, Yohann / Krimm, Isabelle / Crouzy, Serge / Peuchmaur, Marine

European journal of medicinal chemistry

2022 Volume 240, Page(s) 114599

Abstract: Hydrolysis of β-lactam drugs, a major class of antibiotics, by serine or metallo-β-lactamases (SBL or MBL) is one of the main mechanisms for antibiotic resistance. New Delhi Metallo-β-lactamase-1 (NDM-1), an acquired metallo-carbapenemase first reported ... ...

Abstract	Hydrolysis of β-lactam drugs, a major class of antibiotics, by serine or metallo-β-lactamases (SBL or MBL) is one of the main mechanisms for antibiotic resistance. New Delhi Metallo-β-lactamase-1 (NDM-1), an acquired metallo-carbapenemase first reported in 2009, is currently considered one of the most clinically relevant targets for the development of β-lactam-β-lactamase inhibitor combinations active on NDM-producing clinical isolates. Identification of scaffolds that could be further rationally pharmacomodulated to design new and efficient NDM-1 inhibitors is thus urgently needed. Fragment-based drug discovery (FBDD) has become of great interest for the development of new drugs for the past few years and combination of several FBDD strategies, such as virtual and NMR screening, can reduce the drawbacks of each of them independently. Our methodology starting from a high throughput virtual screening on NDM-1 of a large library (more than 700,000 compounds) allowed, after slicing the hit molecules into fragments, to build a targeted library. These hit fragments were included in an in-house untargeted library fragments that was screened by Saturation Transfer Difference (STD) Nuclear Magnetic Resonance (NMR). 37 fragments were finally identified and used to establish a pharmacophore. 10 molecules based on these hit fragments were synthesized to validate our strategy. Indenone 89 that combined two identified fragments shows an inhibitory activity on NDM-1 with a K
MeSH term(s)	Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacology ; Drug Discovery ; beta-Lactamase Inhibitors/chemistry ; beta-Lactamase Inhibitors/pharmacology ; beta-Lactamases/chemistry ; beta-Lactams
Chemical Substances	Anti-Bacterial Agents ; beta-Lactamase Inhibitors ; beta-Lactams ; beta-Lactamases (EC 3.5.2.6) ; beta-lactamase NDM-1 (EC 3.5.2.6)
Language	English
Publishing date	2022-07-11
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2022.114599
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Article: Expanding the chemical space in practice: diversity-oriented synthesis.

Peuchmaur, Marine / Wong, Yung-Sing

Combinatorial chemistry & high throughput screening

2008 Volume 11, Issue 8, Page(s) 587–601

Abstract: Diversity-Oriented Synthesis (DOS) aims to broaden the frontier of accessible collections of complex and diverse small molecules. This review endeavours to dissect the DOS concept through three elements of diversity: building block, stereochemistry, and ... ...

Abstract	Diversity-Oriented Synthesis (DOS) aims to broaden the frontier of accessible collections of complex and diverse small molecules. This review endeavours to dissect the DOS concept through three elements of diversity: building block, stereochemistry, and skeleton. Recent examples in the literature that emphasize the efficient combinations of these elements to generate diversity are reported.
MeSH term(s)	Biomarkers/chemistry ; Combinatorial Chemistry Techniques ; Drug Design ; Molecular Structure ; Signal Transduction ; Stereoisomerism
Chemical Substances	Biomarkers
Language	English
Publishing date	2008-09-05
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	2064785-2
ISSN	1875-5402 ; 1386-2073
ISSN (online)	1875-5402
ISSN	1386-2073
DOI	10.2174/138620708785739916
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