Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB (Q89257069)

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2 April 2020

title

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB (English)

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Mycobacterium tuberculosis

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main subject

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Jennifer Riley

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Laura A T Cleghorn

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Peter C Ray

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Joshua Odingo

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Anuradha Kumar

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Thierry Masquelin

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Abraham Lopez Moure

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Caroline Wilson

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Susan Davis

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Margaret Huggett

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Penelope Turner

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Alasdair Smith

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Ola Epemolu

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Paul Scullion

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Yoko Shishikura

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Liam Ferguson

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Joaquin Rullas

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Laura Guijarro

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Phil Hipskind

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publication date

26 July 2018

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Journal of Medicinal Chemistry

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published in

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volume

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issue

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page(s)

6592-6608

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Crystallographic studies of quinol oxidation site inhibitors: a modified classification of inhibitors for the cytochrome bc(1) complex

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cites work

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12 December 2020

The influence of drug-like concepts on decision-making in medicinal chemistry

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12 December 2020

Discovery of thiophene inhibitors of polo-like kinase

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12 December 2020

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.

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Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis

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Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties

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12 December 2020

Novel Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Anti-malarial Activity in the Mouse Model

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12 December 2020

The challenge of new drug discovery for tuberculosis

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12 December 2020

Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship

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12 December 2020

Getting physical in drug discovery II: the impact of chromatographic hydrophobicity measurements and aromaticity

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12 December 2020

A high-throughput screen to identify inhibitors of ATP homeostasis in non-replicating Mycobacterium tuberculosis

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12 December 2020

Self-assembly driven by an aromatic primary amide motif

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12 December 2020

Lipophilicity in drug discovery

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12 December 2020

Design, synthesis, and X-ray analysis of a glycoconjugate bound to Mycobacterium tuberculosis antigen 85C.

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12 December 2020

Identification of novel imidazo[1,2-a]pyridine inhibitors targeting M. tuberculosis QcrB

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12 December 2020

A dual read-out assay to evaluate the potency of compounds active against Mycobacterium tuberculosis

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12 December 2020

Identification of a small molecule with activity against drug-resistant and persistent tuberculosis

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12 December 2020

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis.

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12 December 2020

Why are membrane targets discovered by phenotypic screens and genome sequencing in Mycobacterium tuberculosis?

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12 December 2020

Tuberculosis drug discovery in the post-post-genomic era

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12 December 2020

Bactericidal activity of an imidazo[1, 2-a]pyridine using a mouse M. tuberculosis infection model

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12 December 2020

Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent

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12 December 2020

Respiratory flexibility in response to inhibition of cytochrome C oxidase in Mycobacterium tuberculosis

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12 December 2020

The WHO 2014 global tuberculosis report--further to go.

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12 December 2020

Perspective: Challenges and opportunities in TB drug discovery from phenotypic screening

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12 December 2020

A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design.

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12 December 2020

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12 December 2020

Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration

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Treatment of Tuberculosis.

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12 December 2020

Improving Drug Design: An Update on Recent Applications of Efficiency Metrics, Strategies for Replacing Problematic Elements, and Compounds in Nontraditional Drug Space

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12 December 2020

Quality guidelines for oral drug candidates: dose, solubility and lipophilicity

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12 December 2020

Stereochemistry Balances Cell Permeability and Solubility in the Naturally Derived Phepropeptin Cyclic Peptides

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12 December 2020

SAR and identification of 2-(quinolin-4-yloxy)acetamides as Mycobacterium tuberculosis cytochrome bc1 inhibitors

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12 December 2020

Improved Phenoxyalkylbenzimidazoles with Activity against Mycobacterium tuberculosis Appear to Target QcrB.

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12 December 2020

Imidazopyridine compounds inhibit mycobacterial growth by depleting ATP levels.

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12 December 2020

10.1021/ACS.JMEDCHEM.8B00172

Identifiers

DOI

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2 April 2020

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PubMed publication ID

29944372

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