Multitargeting Compounds: A Promising Strategy to Overcome Multi-Drug Resistant Tuberculosis

Promiscuous Targets for Antitubercular Drug Discovery: The Paradigm of DprE1 and MmpL3

(2020) Giulia Degiacomi et al.   Applied Sciences-Basel

Direct Inhibition of MmpL3 by Novel Antitubercular Compounds

(2019) Wei Li et al.   ACS Infectious Diseases

Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target

(2019) Bing Zhang et al.   CELL

Cefiderocol: a promising antibiotic against multidrug-resistant Gram-negative bacteria

(2019) Shio-Shin Jean et al.   Expert Review of Anti-Infective Therapy

Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections

(2019) Alex Washburn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Exploration of 5‐(5‐nitrothiophen‐2‐yl)‐4,5‐dihydro‐1H‐pyrazoles as selective, multitargeted antimycobacterial agents

(2019) Neha Agre et al.   Chemical Biology & Drug Design

Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds

(2019) Martin Krátký et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Screening migrants for tuberculosis and latent TB infection: the reward will come later

(2019) Jean-Pierre Zellweger   EUROPEAN RESPIRATORY JOURNAL

Dual-targeted hit identification using pharmacophore screening

(2019) Galyna P. Volynets et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Plasticity of the Mycobacterium tuberculosis respiratory chain and its impact on tuberculosis drug development

(2019) Tiago Beites et al.   Nature Communications

Treatment of Latent Tuberculosis Infection—An Update

(2019) Moises A. Huaman et al.   CLINICS IN CHEST MEDICINE

Multi-Target Antitubercular Drugs

(2018) Jessika de Oliveira Viana et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Affinity-Based Screen for Inhibitors of Bacterial Transglycosylase

(2018) Wei-Shen Wu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK

(2018) Laurent R. Chiarelli et al.   Scientific Reports

Targeting the Proteostasis Network for Mycobacterial Drug Discovery

(2018) Tania J. Lupoli et al.   ACS Infectious Diseases

Prevalence of rifampicin resistant tuberculosis and associated factors among presumptive tuberculosis patients in a secondary referral hospital in Lagos Nigeria

(2018) Olusola Adedeji Adejumo et al.   African Health Sciences

Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis

(2018) Phuong Chi Nguyen et al.   BIOORGANIC CHEMISTRY

Design and synthesis of 5-(5-nitrothiophen-2-yl)-3-phenyl-4,5-dihydro-1H-pyrazole derivatives with improved solubility and potential antituberculosis activity

(2018) Mihir Khambete et al.   Chemical Biology & Drug Design

Development of Multifunctional Molecules as Potential Therapeutic Candidates for Alzheimer’s Disease, Parkinson’s Disease, and Amyotrophic Lateral Sclerosis in the Last Decade

(2018) Masha G. Savelieff et al.   CHEMICAL REVIEWS

Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA)

(2018) Sanofar Abdeen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polypharmacology by Design: A Medicinal Chemist’s Perspective on Multitargeting Compounds

(2018) Ewgenij Proschak et al.   JOURNAL OF MEDICINAL CHEMISTRY

A QSAR and molecular modelling study towards new lead finding: polypharmacological approach to Mycobacterium tuberculosis

(2017) S. Janardhan et al.   SAR AND QSAR IN ENVIRONMENTAL RESEARCH

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors

(2017) Marta Esposito et al.   ACS Infectious Diseases

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles

(2017) Joana Costa-Gouveia et al.   Scientific Reports

Structural Insights into Mycobacterium tuberculosis Rv2671 Protein as a Dihydrofolate Reductase Functional Analogue Contributing to para-Aminosalicylic Acid Resistance

(2016) Yu-Shan Cheng et al.   BIOCHEMISTRY

Salicylanilide N-monosubstituted carbamates: Synthesis and in vitro antimicrobial activity

(2016) Martin Krátký et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Targeting the HSP60/10 chaperonin systems of Trypanosoma brucei as a strategy for treating African sleeping sickness

(2016) Sanofar Abdeen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GroEL/ES inhibitors as potential antibiotics

(2016) Sanofar Abdeen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An unprecedented mechanism of nucleotide methylation in organisms containing thyX

(2016) T. V. Mishanina et al.   SCIENCE

Propargyl-Linked Antifolates Are Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis

(2016) Behnoush Hajian et al.   PLoS One

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG

(2015) Giorgia Mori et al.   CHEMISTRY & BIOLOGY

Multidrug-Resistant Tuberculosis Treatment Outcomes in Relation to Treatment and Initial Versus Acquired Second-Line Drug Resistance

(2015) J. Peter Cegielski et al.   CLINICAL INFECTIOUS DISEASES

Mycobacterium tuberculosis Low Molecular Weight Phosphatases (MPtpA and MPtpB): From Biological Insight to Inhibitors

(2015) Luisa Fanzani et al.   CURRENT MEDICINAL CHEMISTRY

Combating highly resistant emerging pathogen Mycobacterium abscessus and Mycobacterium tuberculosis with novel salicylanilide esters and carbamates

(2015) Zsuzsa Baranyai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and characterization of dual inhibitors against new targets FabG4 and HtdX of Mycobacterium tuberculosis

(2015) Deb Ranjan Banerjee et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tetrahydroisoquinolines affect the whole-cell phenotype of Mycobacterium tuberculosis by inhibiting the ATP-dependent MurE ligase

(2015) Juan D. Guzman et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Nonracemic Antifolates Stereoselectively Recruit Alternate Cofactors and Overcome Resistance in S. aureus

(2015) Santosh Keshipeddy et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Principles in the design of ligand-targeted cancer therapeutics and imaging agents

(2015) Madduri Srinivasarao et al.   NATURE REVIEWS DRUG DISCOVERY

Multi-target pharmacology: possibilities and limitations of the “skeleton key approach” from a medicinal chemist perspective

(2015) Alan Talevi   Frontiers in Pharmacology

Advances in Mycobacterial Isocitrate Lyase Targeting and Inhibitors

(2015) M. Kratky et al.   CURRENT MEDICINAL CHEMISTRY

Novel Insights into the Mechanism of Inhibition of MmpL3, a Target of Multiple Pharmacophores in Mycobacterium tuberculosis

(2014) Wei Li et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Assessment of Mycobacterium tuberculosis Pantothenate Kinase Vulnerability through Target Knockdown and Mechanistically Diverse Inhibitors

(2014) B. K. Kishore Reddy et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Using the reversible inhibition of gastric lipase by Orlistat for investigating simultaneously lipase adsorption and substrate hydrolysis at the lipid–water interface

(2014) Anaïs Bénarouche et al.   BIOCHIMIE

Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates

(2014) Martin Krátký et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A biochemical screen for GroEL/GroES inhibitors

(2014) Steven M. Johnson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Folate Pathway Disruption Leads to Critical Disruption of Methionine Derivatives in Mycobacterium tuberculosis

(2014) Molly R. Nixon et al.   CHEMISTRY & BIOLOGY

Multifunctional compounds: Smart molecules for multifactorial diseases

(2014) Yogita Bansal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches

(2014) Baptiste Villemagne et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multitarget Drug Discovery for Tuberculosis and Other Infectious Diseases

(2014) Kai Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polypharmacology: Challenges and Opportunities in Drug Discovery

(2014) Andrew Anighoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes

(2014) Martin Krátký et al.   TheScientificWorldJOURNAL

Characterizing the pocketome of Mycobacterium tuberculosis and application in rationalizing polypharmacological target selection

(2014) Praveen Anand et al.   Scientific Reports

Advances in the development of new tuberculosis drugs and treatment regimens

(2013) Alimuddin Zumla et al.   NATURE REVIEWS DRUG DISCOVERY

SQ109 Targets MmpL3, a Membrane Transporter of Trehalose Monomycolate Involved in Mycolic Acid Donation to the Cell Wall Core of Mycobacterium tuberculosis

(2012) Kapil Tahlan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mycobacterial lipolytic enzymes: A gold mine for tuberculosis research

(2012) L. Dedieu et al.   BIOCHIMIE

Structure–activity relationships of antitubercular salicylanilides consistent with disruption of the proton gradient via proton shuttling

(2012) Ill-Young Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Multitarget ligands in antibacterial research: progress and opportunities

(2012) Stephen P East et al.   Expert Opinion on Drug Discovery

Discovery and development of SQ109: a new antitubercular drug with a novel mechanism of action

(2012) Katherine A Sacksteder et al.   Future Microbiology

The Antifolates

(2012) Michele Visentin et al.   HEMATOLOGY-ONCOLOGY CLINICS OF NORTH AMERICA

Salicylanilide derivatives block Mycobacterium tuberculosis through inhibition of isocitrate lyase and methionine aminopeptidase

(2012) Martin Krátký et al.   TUBERCULOSIS

MmpL3 Is the Cellular Target of the Antitubercular Pyrrole Derivative BM212

(2011) Valentina La Rosa et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Ethionamide Boosters: Synthesis, Biological Activity, and Structure−Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors

(2011) Marion Flipo et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-throughput identification of antibacterials against methicillin-resistant Staphylococcus aureus (MRSA) and the transglycosylase

(2010) Ting-Jen Rachel Cheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Antimycobacterial activity of new 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-one derivatives. Molecular modeling investigations

(2009) Daniele Zampieri et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Salicylanilide carbamates: Antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains

(2009) Juana M. Férriz et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Multitarget drugs: the present and the future of cancer therapy

(2009) Annalisa Petrelli et al.   EXPERT OPINION ON PHARMACOTHERAPY

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

(2009) Nicolas Willand et al.   NATURE MEDICINE

ATP competitive inhibitors of d-alanine–d-alanine ligase based on protein kinase inhibitor scaffolds

(2008) Gemma Triola et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Mycobacterium tuberculosis Mutant Lacking the groEL Homologue cpn60.1 Is Viable but Fails To Induce an Inflammatory Response in Animal Models of Infection

(2008) Y. Hu et al.   INFECTION AND IMMUNITY