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Challenging the Drug-Likeness Dogma for New Drug Discovery in Tuberculosis

Frontiers in microbiology, 2018-07, Vol.9, p.1367-1367

2018

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Indoleamides are active against drug-resistant Mycobacterium tuberculosis

Nature communications, 2013-12, Vol.4 (1), Article 2907

2013

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Preliminary Structure–Activity Relationships and Biological Evaluation of Novel Antitubercular Indolecarboxamide Derivatives Against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains

Journal of medicinal chemistry, 2013-05, Vol.56 (10), p.4093-4103

2013

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Inhibitors of the sulfur assimilation pathway in bacterial pathogens as enhancers of antibiotic therapy

Current medicinal chemistry, 2015-01, Vol.22 (2), p.187-213

2015

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Cycloserine enantiomers are reversible inhibitors of human alanine:glyoxylate aminotransferase: implications for Primary Hyperoxaluria type 1

Biochemical journal, 2019-12, Vol.476 (24), p.3751-3768

2019

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Sodium Hyaluronate Nanocomposite Respirable Microparticles to Tackle Antibiotic Resistance with Potential Application in Treatment of Mycobacterial Pulmonary Infections

Pharmaceutics, 2019-05, Vol.11 (5), p.203

2019

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Nitric oxide-releasing cyclodextrins as biodegradable antibacterial scaffolds: a patent evaluation of US2019343869(A1)

Expert opinion on therapeutic patents, 2020-12, Vol.30 (12), p.901-905

Pieroni, Marco

2020

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Inhibitors of O-Acetylserine Sulfhydrylase with a Cyclopropane-Carboxylic Acid Scaffold Are Effective Colistin Adjuvants in Gram Negative Bacteria

Pharmaceuticals (Basel, Switzerland), 2022-06, Vol.15 (6), p.766

2022

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Refining the structure−activity relationships of 2-phenylcyclopropane carboxylic acids as inhibitors of O-acetylserine sulfhydrylase isoforms

Journal of enzyme inhibition and medicinal chemistry, 2019-01, Vol.34 (1), p.31-43

2019

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Discovery of Substituted (2-Aminooxazol-4-yl)Isoxazole-3-carboxylic Acids as Inhibitors of Bacterial Serine Acetyltransferase in the Quest for Novel Potential Antibacterial Adjuvants

Pharmaceuticals (Basel, Switzerland), 2021-02, Vol.14 (2), p.174

2021

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Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand-based drug design

Journal of enzyme inhibition and medicinal chemistry, 2018-01, Vol.33 (1), p.1444-1452

2018

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Discovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases

Journal of enzyme inhibition and medicinal chemistry, 2018-01, Vol.33 (1), p.1537-1544

2018

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A Competitive O-Acetylserine Sulfhydrylase Inhibitor Modulates the Formation of Cysteine Synthase Complex

Catalysts, 2021-06, Vol.11 (6), p.700

2021

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Efflux Activity Differentially Modulates the Levels of Isoniazid and Rifampicin Resistance among Multidrug Resistant and Monoresistant Mycobacterium tuberculosis Strains

Antibiotics (Basel), 2018-03, Vol.7 (1), p.18

2018

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Synthesis of 7-Desmethyl Analogs of (+)- and (−)-Huperzine A

Heterocycles, 2015, Vol.91 (12), p.2285

2015

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Exploring the chemical space around N-(5-nitrothiazol-2-yl)-1,2,3-thiadiazole-4-carboxamide, a hit compound with serine acetyltransferase (SAT) inhibitory properties

Results in Chemistry, 2022-01, Vol.4, p.100443, Article 100443

2022

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Pyrido[1,2-a]benzimidazole-Based Agents Active Against Tuberculosis (TB), Multidrug-Resistant (MDR) TB and Extensively Drug-Resistant (XDR) TB

ChemMedChem, 2011-02, Vol.6 (2), p.334-342

2011

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Novel N-Benzoyl-2-Hydroxybenzamide Disrupts Unique Parasite Secretory Pathway

Antimicrobial Agents and Chemotherapy, 2012-05, Vol.56 (5), p.2666-2682

2012

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Derivatives of 3-isoxazolecarboxylic acid esters: a potent and selective compound class against replicating and nonreplicating Mycobacterium tuberculosis

Current topics in medicinal chemistry, 2012-04, Vol.12 (7), p.729-734

2012

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Biochemical Characterization of Aspergillus fumigatus AroH, a Putative Aromatic Amino Acid Aminotransferase

Frontiers in molecular biosciences, 2018-11, Vol.5, p.104-104

2018

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Spectinamides: a challenge, a proof, and a suggestion

Trends in microbiology (Regular ed.), 2014-04, Vol.22 (4), p.170-171

2014

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Identification of Human Alanine–Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1

Journal of medicinal chemistry, 2022-07, Vol.65 (14), p.9718-9734

2022

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Substituted N‑Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery

Journal of medicinal chemistry, 2017-08, Vol.60 (16), p.7108-7122

2017

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Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure–Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents

Journal of medicinal chemistry, 2017-03, Vol.60 (5), p.1959-1970

2017

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Mutation of Rv2887, a marR-like gene, confers Mycobacterium tuberculosis resistance to an imidazopyridine-based agent

Antimicrobial agents and chemotherapy, 2015-11, Vol.59 (11), p.6873-6881

2015

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Challenging the Drug-Likeness Dogma for New Drug Discovery in Tuberculosis

Indoleamides are active against drug-resistant Mycobacterium tuberculosis

Preliminary Structure–Activity Relationships and Biological Evaluation of Novel Antitubercular Indolecarboxamide Derivatives Against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains

Inhibitors of the sulfur assimilation pathway in bacterial pathogens as enhancers of antibiotic therapy

Cycloserine enantiomers are reversible inhibitors of human alanine:glyoxylate aminotransferase: implications for Primary Hyperoxaluria type 1

Sodium Hyaluronate Nanocomposite Respirable Microparticles to Tackle Antibiotic Resistance with Potential Application in Treatment of Mycobacterial Pulmonary Infections

Nitric oxide-releasing cyclodextrins as biodegradable antibacterial scaffolds: a patent evaluation of US2019343869(A1)

Inhibitors of O-Acetylserine Sulfhydrylase with a Cyclopropane-Carboxylic Acid Scaffold Are Effective Colistin Adjuvants in Gram Negative Bacteria

Refining the structure−activity relationships of 2-phenylcyclopropane carboxylic acids as inhibitors of O-acetylserine sulfhydrylase isoforms

Discovery of Substituted (2-Aminooxazol-4-yl)Isoxazole-3-carboxylic Acids as Inhibitors of Bacterial Serine Acetyltransferase in the Quest for Novel Potential Antibacterial Adjuvants

Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand-based drug design

Discovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases

A Competitive O-Acetylserine Sulfhydrylase Inhibitor Modulates the Formation of Cysteine Synthase Complex

Efflux Activity Differentially Modulates the Levels of Isoniazid and Rifampicin Resistance among Multidrug Resistant and Monoresistant Mycobacterium tuberculosis Strains

Synthesis of 7-Desmethyl Analogs of (+)- and (−)-Huperzine A

Exploring the chemical space around N-(5-nitrothiazol-2-yl)-1,2,3-thiadiazole-4-carboxamide, a hit compound with serine acetyltransferase (SAT) inhibitory properties

Pyrido[1,2-a]benzimidazole-Based Agents Active Against Tuberculosis (TB), Multidrug-Resistant (MDR) TB and Extensively Drug-Resistant (XDR) TB

Novel N-Benzoyl-2-Hydroxybenzamide Disrupts Unique Parasite Secretory Pathway

Derivatives of 3-isoxazolecarboxylic acid esters: a potent and selective compound class against replicating and nonreplicating Mycobacterium tuberculosis

Biochemical Characterization of Aspergillus fumigatus AroH, a Putative Aromatic Amino Acid Aminotransferase

Spectinamides: a challenge, a proof, and a suggestion

Identification of Human Alanine–Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1

Substituted N‑Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery

Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure–Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents

Mutation of Rv2887, a marR-like gene, confers Mycobacterium tuberculosis resistance to an imidazopyridine-based agent

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