Antituberculosis Drug Research: A Critical Overview

Linezolid, the first oxazolidinone antibacterial agent

(2011) Karen L. Leach et al.   Annals of the New York Academy of Sciences

In VivoPharmacodynamics of Torezolid Phosphate (TR-701), a New Oxazolidinone Antibiotic, against Methicillin-Susceptible and Methicillin-Resistant Staphylococcus aureus Strains in a Mouse Thigh Infection Model

(2011) Arnold Louie et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synergistic Drug Combinations for Tuberculosis Therapy Identified by a Novel High-Throughput Screen

(2011) Santiago Ramón-García et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

New 1,4-di-N-oxide-quinoxaline-2-ylmethylene isonicotinic acid hydrazide derivatives as anti-Mycobacterium tuberculosis agents

(2011) Enrique Torres et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Anti-tubercular agents. Part 6: Synthesis and antimycobacterial activity of novel arylsulfonamido conjugated oxazolidinones

(2011) Ahmed Kamal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Molecular basis and mechanisms of drug resistance in Mycobacterium tuberculosis: classical and new drugs

(2011) P. E. Almeida Da Silva et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Synthesis and Structure–Activity Relationships of Varied Ether Linker Analogues of the Antitubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

(2011) Andrew M. Thompson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Current Status and Research Strategies in Tuberculosis Drug Development

(2011) Lynn G. Dover et al.   JOURNAL OF MEDICINAL CHEMISTRY

A 2020 vision for vaccines against HIV, tuberculosis and malaria

(2011) Rino Rappuoli et al.   NATURE

Development of vaccines against tuberculosis

(2011) Anil K. Tyagi et al.   TUBERCULOSIS

The BCG World Atlas: A Database of Global BCG Vaccination Policies and Practices

(2011) Alice Zwerling et al.   PLOS MEDICINE

Clinical Isolates of Mycobacterium tuberculosis in Four European Hospitals Are Uniformly Susceptible to Benzothiazinones

(2010) M. R. Pasca et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

PA-824 Exhibits Time-Dependent Activity in a Murine Model of Tuberculosis

(2010) Zahoor Ahmad et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Interaction studies of novel cell selective antimicrobial peptides with model membranes and E. coli ATCC 11775

(2010) Seema Joshi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines

(2010) José C. Aponte et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas

(2010) Carlos Nava-Zuazo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: Novel antibacterial agents against Mycobacterium tuberculosis

(2010) Xiaokai Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824

(2010) Soledad Bollo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of Mycobacterium tuberculosis clinical isolates in Bangladesh by a species distinguishable multiplex PCR

(2010) Chie Nakajima et al.   BMC INFECTIOUS DISEASES

Tuberculosis Immunity: Opportunities from Studies with Cattle

(2010) W. Ray Waters et al.   Clinical & Developmental Immunology

Synthesis and evaluation of SQ109 analogues as potential anti-tuberculosis candidates

(2010) Oluseye K. Onajole et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A bioactive labdane diterpenoid from Curcuma amada and its semisynthetic analogues as antitubercular agents

(2010) Sailendra Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Schiff bases of indoline-2,3-dione (isatin) derivatives and nalidixic acid carbohydrazide, synthesis, antitubercular activity and pharmacophoric model building

(2010) Tarek Aboul-Fadl et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, antimicrobial activity and structure–activity relationship study of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives

(2010) Mukul Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thioridazine cures extensively drug-resistant tuberculosis (XDR-TB) and the need for global trials is now!

(2010) Leonard Amaral et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Pulmonary tuberculosis due to Mycobacterium microti: a study of six recent cases in France

(2010) G. Panteix et al.   JOURNAL OF MEDICAL MICROBIOLOGY

Synthesis and Structure−Activity Relationships of Aza- and Diazabiphenyl Analogues of the Antitubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

(2010) Iveta Kmentova et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Trisubstituted Benzimidazoles, TargetingMtbFtsZ, as a New Class of Antitubercular Agents

(2010) Kunal Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Eucapsitrione, an Anti-Mycobacterium tuberculosisAnthraquinone Derivative from the Cultured Freshwater CyanobacteriumEucapsissp.

(2010) Megan Sturdy et al.   JOURNAL OF NATURAL PRODUCTS

Anthraquinone, Cyclopentanone, and Naphthoquinone Derivatives from the Sea Fan-Derived FungiFusariumspp. PSU-F14 and PSU-F135

(2010) Kongkiat Trisuwan et al.   JOURNAL OF NATURAL PRODUCTS

Benzothiazinones: Prodrugs That Covalently Modify the Decaprenylphosphoryl-β-d-ribose 2′-epimerase DprE1 ofMycobacterium tuberculosis

(2010) Claudia Trefzer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Tetraoxanes: Synthetic and Medicinal Chemistry Perspective

(2010) Nitin Kumar et al.   MEDICINAL RESEARCH REVIEWS

Conformationally-constrained indeno[2,1-c]quinolines – a new class of anti-mycobacterial agents

(2010) Ram Shankar Upadhayaya et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

The Antipsychotic Thioridazine Shows Promising Therapeutic Activity in a Mouse Model of Multidrug-Resistant Tuberculosis

(2010) Dick van Soolingen et al.   PLoS One

Bactericidal activity of the diarylquinoline TMC207 against Mycobacterium tuberculosis outside and within cells

(2010) Jasvir Dhillon et al.   TUBERCULOSIS

The use of anti-tuberculosis therapy for latent TB infection

(2010) Justin Denholm   Infection and Drug Resistance

Safety, Tolerability, and Pharmacokinetics of PA-824 in Healthy Subjects

(2009) A. M. Ginsberg et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis and in vitro antitubercular activity of a series of quinoline derivatives

(2009) Marcus V.N. de Souza et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure–activity relationship studies

(2009) Sandra Gemma et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel triazole, urea and thiourea derivatives of quinoline against Mycobacterium tuberculosis

(2009) Ram Shankar Upadhayaya et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives

(2009) André L.P. Candéa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis

(2009) Esther del Olmo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis of novel [1,2]-diamines with antituberculosis activity

(2009) Qingyi Meng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and antibacterial activity evaluation of metronidazole–triazole conjugates

(2009) Beena et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antitubercular activity of α,ω-diaminoalkanes, H2N(CH2)nNH2

(2009) Fátima M.F. Vergara et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of (S,S)-N,N′-bis-[3-(2,2′,6,6′-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity

(2009) Xuelian Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents

(2009) Sumesh Eswaran et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and antibacterial activity of benzyl-[3-(benzylamino-methyl)-cyclohexylmethyl]-amine derivatives

(2009) Deepak Kumar et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The methods of synthesis, modification, and biological activity of 4-quinolones (review)

(2009) A. A. Boteva et al.   Chemistry of Heterocyclic Compounds

A microwave-assisted, facile, regioselective Friedländer synthesis and antitubercular evaluation of 2,9-diaryl-2,3-dihydrothieno-[3,2- b ]quinolines

(2009) Kamaraj Balamurugan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of benzofuro[2,3- b ]quinoline derivatives as a new class of antituberculosis agents

(2009) Chiao-Li Yang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Antituberculosis activity of alkylated mulinane diterpenoids

(2009) Gloria María Molina-Salinas et al.   FITOTERAPIA

Antituberculosis activity of natural and semisynthetic azorellane and mulinane diterpenoids

(2009) Gloria María Molina-Salinas et al.   FITOTERAPIA

Schiff Bases as Potential Fungicides and Nitrification Inhibitors

(2009) Nisha Aggarwal et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Antimycobacterial terpenoids from Juniperus communis L. (Cuppressaceae)

(2009) Andréa Y. Gordien et al.   JOURNAL OF ETHNOPHARMACOLOGY

From Serendipity to Rational Antituberculosis Drug Discovery of Mefloquine-Isoxazole Carboxylic Acid Esters

(2009) Jialin Mao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Searching for New Cures for Tuberculosis: Design, Synthesis, and Biological Evaluation of 2-Methylbenzothiazoles

(2009) Qingqing Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationships of Antitubercular Nitroimidazoles. 1. Structural Features Associated with Aerobic and Anaerobic Activities of 4- and 5-Nitroimidazoles

(2009) Pilho Kim et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationships for a Series of Quinoline-Based Compounds Active against Replicating and NonreplicatingMycobacterium tuberculosis

(2009) Annamaria Lilienkampf et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Structure−activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains

(2009) Hamish S. Sutherland et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Structure−Activity Studies of Biphenyl Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

(2009) Brian D. Palmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis

(2009) V. Makarov et al.   SCIENCE

Effect of pyrazinamidase activity on pyrazinamide resistance in Mycobacterium tuberculosis

(2009) Patricia Sheen et al.   TUBERCULOSIS

Progress in understanding the human immune responses to Mycobacterium tuberculosis

(2009) Peter F. Barnes et al.   TUBERCULOSIS

Evaluation of new vaccines for tuberculosis in the guinea pig model

(2009) Ann Williams et al.   TUBERCULOSIS

Discovery and validation of new antitubercular compounds as potential drug leads and probes

(2009) Robert C. Goldman et al.   TUBERCULOSIS

High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv

(2009) Subramaniam Ananthan et al.   TUBERCULOSIS

Mycobacterium abscessusandM. aviumTrigger Toll-Like Receptor 2 and Distinct Cytokine Response in Human Cells

(2008) Elizabeth P. Sampaio et al.   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

Early Bactericidal Activity and Pharmacokinetics of the Diarylquinoline TMC207 in Treatment of Pulmonary Tuberculosis

(2008) R. Rustomjee et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Design and SAR of new substituted purines bearing aryl groups at N9 position as HIV-1 Tat–TAR interaction inhibitors

(2008) Ruifang Pang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824

(2008) Xiaojin Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tuberculosis in Africa: Learning from Pathogenesis for Biomarker Identification

(2008) Stefan H.E. Kaufmann et al.   Cell Host & Microbe

Hydronaphthalenones and a Dihydroramulosin from the Endophytic Fungus PSU-N24

(2008) Ubonta Sommart et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

New anti-tuberculosis drugs in clinical trials with novel mechanisms of action

(2008) Emma C. Rivers et al.   DRUG DISCOVERY TODAY

A macrolactone from benzo[a]phenazine with potent activity against Mycobacterium tuberculosis

(2008) Raphael S.F. Silva et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The TB laboratory of the future: macrophage-based selection of XDR-TB therapeutics

(2008) Marta Martins et al.   Future Microbiology

Tuberculous Granulomas Are Hypoxic in Guinea Pigs, Rabbits, and Nonhuman Primates

(2008) L. E. Via et al.   INFECTION AND IMMUNITY

Synthesis, Reduction Potentials, and Antitubercular Activity of Ring A/B Analogues of the Bioreductive Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

(2008) Andrew M. Thompson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal structures of oseltamivir-resistant influenza virus neuraminidase mutants

(2008) Patrick J. Collins et al.   NATURE

The oxazolidinone antibiotics perturb the ribosomal peptidyl-transferase center and effect tRNA positioning

(2008) D. N. Wilson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

SQ109

(2008)   TUBERCULOSIS

Thioridazine

(2008)   TUBERCULOSIS

Strategies of extensively drug-resistant TB risk management for health workers and other care givers

(2008) Chiang Chen-Yuan et al.   Expert Review of Respiratory Medicine

Synthesis and anti-mycobacterial activity of (E)-N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives

(2007) Maria Cristina da Silva Lourenço et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Pharmacodynamics and pharmacokinetics of SQ109, a new diamine-based antitubercular drug

(2004) Lee Jia et al.   BRITISH JOURNAL OF PHARMACOLOGY