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Advances in the discovery of N-acylethanolamine acid amidase inhibitors

Pharmacological research, 2014-08, Vol.86, p.11-17

2014

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Synthesis and Structure–Activity Relationship (SAR) of 2‑Methyl-4-oxo-3-oxetanylcarbamic Acid Esters, a Class of Potent N‑Acylethanolamine Acid Amidase (NAAA) Inhibitors

Journal of medicinal chemistry, 2013-09, Vol.56 (17), p.6917-6934

2013

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A European regulatory perspective on cystic fibrosis: current treatments, trends in drug development and translational challenges for CFTR modulators

European respiratory review, 2018-06, Vol.27 (148), p.170124

2018

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Synthesis, Structure-Activity, and Structure-Stability Relationships of 2-Substituted-N-(4-oxo-3-oxetanyl) N-Acylethanolamine Acid Amidase (NAAA) Inhibitors

ChemMedChem, 2014-02, Vol.9 (2), p.323-336

2014

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Promoting Safe Early Clinical Research of Novel Drug Candidates: A European Union Regulatory Perspective

Clinical pharmacology and therapeutics, 2018-04, Vol.103 (4), p.564-566

2018

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EMA commentary on the ICH guideline for testing for carcinogenicity of pharmaceuticals

British journal of clinical pharmacology, 2023-08, Vol.89 (8), p.2341-2348

2023

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Discovery and SAR Evolution of Pyrazole Azabicyclo[3.2.1]octane Sulfonamides as a Novel Class of Non-Covalent N‑Acylethanolamine-Hydrolyzing Acid Amidase (NAAA) Inhibitors for Oral Administration

Journal of medicinal chemistry, 2021-09, Vol.64 (18), p.13327-13355

2021

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Activity-Based Probe for N‑Acylethanolamine Acid Amidase

ACS chemical biology, 2015-09, Vol.10 (9), p.2057-2064

2015

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Safety Pharmacology Study Results and their Impact on the Design of First.in.human Trials for Authorised Oncology Therapies

Pharmaceutical medicine, 2018-10, Vol.32 (5), p.335-341

2018

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2-Oxopyridine-1-carboxylates, highly reactive carbamoylating agents of β-hydroxy α-aminoacids

Tetrahedron letters, 2015-05, Vol.56 (22), p.2887-2891

2015

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Synthesis of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural productsElectronic supplementary information (ESI) available: The synthesis procedures for compounds 4 to 9 are included in the ESI as Document S1. The protocol for the anticancer activity in vitro testing is also included as Document S2. The spectra of all compounds described in the present work (IR, 1H NMR, 13C NMR, DEPT, COSY, HSQC and MS) are included in the ESI as Document S3. CCDC 1562215. For ESI and crysta

2018-02

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Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure–activity relationship (SAR) studies

European journal of medicinal chemistry, 2016-03, Vol.111, p.138-159

2016

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Design and synthesis of new antitumor agents with the 1,7-epoxycyclononane framework. Study of their anticancer action mechanism by a model compound

Bioorganic & medicinal chemistry, 2018-07, Vol.26 (12), p.3379-3398

2018

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Novel activity-based probes for N-acylethanolamine acid amidase

Chemical communications (Cambridge, England), 2017-08, Vol.53 (86), p.11810-11813

2017

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Correction: Synthesis of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural products

Organic & biomolecular chemistry, 2018-03, Vol.16 (13), p.2362-2362

2018

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Synthesis, Biological Evaluation, and 3D QSAR Study of 2‑Methyl-4-oxo-3-oxetanylcarbamic Acid Esters as N‑Acylethanolamine Acid Amidase (NAAA) Inhibitors

Journal of medicinal chemistry, 2014-12, Vol.57 (23), p.10101-10111

2014

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Synthesis of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural products

Organic & biomolecular chemistry, 2018-03, Vol.16 (9), p.1557-1580

2018

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Safety Pharmacology Study Results and their Impact on the Design of First-in-human Trials for Authorised Oncology Therapies

Pharmaceutical medicine, 2018-10, Vol.32 (5), p.335-341

2018

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Novel activity-based probes for N-acylethanolamine acid amidaseElectronic supplementary information (ESI) available: Experimental procedures, supplementary figures. See DOI: 10.1039/c7cc06838g

2017-08

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Response to: “The Role of Quantitative Systems Pharmacology in the Design of First‐in‐Human Trials”

Clinical pharmacology and therapeutics, 2018-11, Vol.104 (5), p.798-798

2018

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Synthesis of 1,7-epoxycyclononanes and 1,8-epoxycyclodecanes by β-fragmentation reactions using LTA and I2

Tetrahedron letters, 2006-11, Vol.47 (47), p.8299-8304

2006

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Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Journal of visualized experiments, 2016-11 (117)

2016

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Unprecedented double benzylic rearrangement: regio- and stereospecific tandem 1,4-shift and Curtin rearrangement

Tetrahedron, 2012-09, Vol.68 (39), p.8276-8285

2012

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Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Journal of visualized experiments, 2016-11 (117)

2016

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β-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine

ACS medicinal chemistry letters, 2012-05, Vol.3 (5), p.422-426

2012

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Advances in the discovery of N-acylethanolamine acid amidase inhibitors

Synthesis and Structure–Activity Relationship (SAR) of 2‑Methyl-4-oxo-3-oxetanylcarbamic Acid Esters, a Class of Potent N‑Acylethanolamine Acid Amidase (NAAA) Inhibitors

A European regulatory perspective on cystic fibrosis: current treatments, trends in drug development and translational challenges for CFTR modulators

Synthesis, Structure-Activity, and Structure-Stability Relationships of 2-Substituted-N-(4-oxo-3-oxetanyl) N-Acylethanolamine Acid Amidase (NAAA) Inhibitors

Promoting Safe Early Clinical Research of Novel Drug Candidates: A European Union Regulatory Perspective

EMA commentary on the ICH guideline for testing for carcinogenicity of pharmaceuticals

Discovery and SAR Evolution of Pyrazole Azabicyclo[3.2.1]octane Sulfonamides as a Novel Class of Non-Covalent N‑Acylethanolamine-Hydrolyzing Acid Amidase (NAAA) Inhibitors for Oral Administration

Activity-Based Probe for N‑Acylethanolamine Acid Amidase

Safety Pharmacology Study Results and their Impact on the Design of First.in.human Trials for Authorised Oncology Therapies

2-Oxopyridine-1-carboxylates, highly reactive carbamoylating agents of β-hydroxy α-aminoacids

Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure–activity relationship (SAR) studies

Design and synthesis of new antitumor agents with the 1,7-epoxycyclononane framework. Study of their anticancer action mechanism by a model compound

Novel activity-based probes for N-acylethanolamine acid amidase

Correction: Synthesis of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural products

Synthesis, Biological Evaluation, and 3D QSAR Study of 2‑Methyl-4-oxo-3-oxetanylcarbamic Acid Esters as N‑Acylethanolamine Acid Amidase (NAAA) Inhibitors

Synthesis of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural products

Safety Pharmacology Study Results and their Impact on the Design of First-in-human Trials for Authorised Oncology Therapies

Novel activity-based probes for N-acylethanolamine acid amidaseElectronic supplementary information (ESI) available: Experimental procedures, supplementary figures. See DOI: 10.1039/c7cc06838g

Response to: “The Role of Quantitative Systems Pharmacology in the Design of First‐in‐Human Trials”

Synthesis of 1,7-epoxycyclononanes and 1,8-epoxycyclodecanes by β-fragmentation reactions using LTA and I2

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Unprecedented double benzylic rearrangement: regio- and stereospecific tandem 1,4-shift and Curtin rearrangement

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

β-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine

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