New agents for the treatment of drug-resistant Mycobacterium tuberculosis
TLDR
The challenges to developing drugs to treat tuberculosis are discussed and how the field has adapted to these difficulties, with an emphasis on drug discovery approaches that might produce more effective agents and treatment regimens.About:
This article is published in Advanced Drug Delivery Reviews.The article was published on 2016-07-01 and is currently open access. It has received 262 citations till now. The article focuses on the topics: Bedaquiline & Tuberculosis.read more
Citations
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Recent updates on drug resistance in Mycobacterium tuberculosis
Richa Singh,Surya Prakash Dwivedi,Usha Singh Gaharwar,Ramovatar Meena,Paulraj Rajamani,Tulika Prasad +5 more
TL;DR: The aim of this review is to provide recent updates on drug resistance mechanisms, newly developed/repurposed anti‐TB agents in pipeline and international recommendations to manage MDR‐TB, based on recent literature and WHO guidelines and aims to facilitate better understanding of drug resistance for effective TB therapy and clinical management.
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Challenges and recent progress in drug discovery for tropical diseases
TL;DR: Some of the challenges involved in developing new drugs to treatfectious tropical diseases are discussed, and there is still a long way to go.
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Narrow-Spectrum Antibacterial Agents.
TL;DR: The advantages and challenges of narrow-Spectrum antibacterial agents are outlined, the progress that has been made toward developing diagnostics to enable their use is discussed, and some of the narrow-spectrum antib bacterial agents currently being investigated against some ofThe most clinically important bacteria including Clostridium difficile, Mycobacterium tuberculosis and several ESKAPE pathogens are described.
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New drugs and perspectives for new anti-tuberculosis regimens.
Simon Tiberi,Marcela Muñoz-Torrico,Raquel Duarte,Margareth Pretti Dalcolmo,Lia D'Ambrosio,Giovanni Battista Migliori +5 more
TL;DR: An update on the new drugs and perspectives for the treatment of drug-susceptible and drug-resistant tuberculosis is given.
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Thinking Outside the Box-Novel Antibacterials To Tackle the Resistance Crisis.
TL;DR: This Review encompasses several aspects of the antibiotic development pipeline from very early strategies to mature drugs, and aims to connect innovative antimicrobial approaches to stimulate interdisciplinary partnerships between chemists from academia and industry.
References
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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
TL;DR: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described in this article, where the rule of 5 is used to predict poor absorption or permeability when there are more than 5 H-bond donors, 10 Hbond acceptors, and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415).
Journal ArticleDOI
Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence
Stewart T. Cole,Roland Brosch,Julian Parkhill,Thierry Garnier,Carol Churcher,David Harris,Stephen V. Gordon,Karin Eiglmeier,S. Gas,Clifton E. Barry,Fredj Tekaia,K. Badcock,D. Basham,D. Brown,Tracey Chillingworth,R. Connor,Robert L. Davies,K. Devlin,Theresa Feltwell,S. Gentles,N. Hamlin,S. Holroyd,T. Hornsby,Kay Jagels,Anders Krogh,J. McLean,Sharon Moule,Lee Murphy,K. Oliver,J. Osborne,Michael A. Quail,Marie-Adèle Rajandream,Jane Rogers,S. Rutter,K. Seeger,Jason Skelton,Rob Squares,S. Squares,John Sulston,K. Taylor,Sally Whitehead,Bart Barrell +41 more
TL;DR: The complete genome sequence of the best-characterized strain of Mycobacterium tuberculosis, H37Rv, has been determined and analysed in order to improve the understanding of the biology of this slow-growing pathogen and to help the conception of new prophylactic and therapeutic interventions.
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Drug-like properties and the causes of poor solubility and poor permeability
TL;DR: There are currently about 10000 drug-like compounds, and true diversity does not exist in experimental combinatorial chemistry screening libraries because current ADME experimental screens are multi-mechanisms, and predictions get worse as more data accumulates.
Journal ArticleDOI
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
Koen Andries,Peter Verhasselt,Jerome Guillemont,Hinrich W. H. Göhlmann,Jean-Marc Neefs,Hans Winkler,Jef Van Gestel,Philip Timmerman,Min Zhu,Ennis Lee,Peter Williams,Didier de Chaffoy,Emma Huitric,Sven Hoffner,Emmanuelle Cambau,Chantal Truffot-Pernot,Nacer Lounis,Vincent Jarlier +17 more
TL;DR: A diarylquinoline, R207910, is identified that potently inhibits both drug-sensitive and drug-resistant Mycobacterium tuberculosis in vitro and mutants selected in vitro suggest that the drug targets the proton pump of adenosine triphosphate (ATP) synthase.
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Drug–target residence time and its implications for lead optimization
TL;DR: The potential advantages of long residence time in terms of duration of pharmacological effect and target selectivity are described, as quantified by the dissociative half-life of the drug–target binary complex.
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