Relevant bibliographies by topics / DprE1 inhibitors

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  1. Journal articles
  2. Dissertations / Theses

Academic literature on the topic 'DprE1 inhibitors'

Author: Grafiati
Published: 4 June 2021
Last updated: 18 February 2022

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Journal articles on the topic "DprE1 inhibitors"

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Foo, Caroline Shi-Yan, Benoit Lechartier, Gaëlle S. Kolly, et al. "Characterization of DprE1-Mediated Benzothiazinone Resistance in Mycobacterium tuberculosis." Antimicrobial Agents and Chemotherapy 60, no. 11 (2016): 6451–59. http://dx.doi.org/10.1128/aac.01523-16.

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ABSTRACTBenzothiazinones (BTZs) are a class of compounds found to be extremely potent against both drug-susceptible and drug-resistantMycobacterium tuberculosisstrains. The potency of BTZs is explained by their specificity for their target decaprenylphosphoryl-d-ribose oxidase (DprE1), in particular by covalent binding of the activated form of the compound to the critical cysteine 387 residue of the enzyme. To probe the role of C387, we used promiscuous site-directed mutagenesis to introduce other codons at this position intodprE1ofM. tuberculosis. The resultant viable BTZ-resistant mutants we
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Makarov, Vadim, João Neres, Ruben C. Hartkoorn, et al. "The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis." Antimicrobial Agents and Chemotherapy 59, no. 8 (2015): 4446–52. http://dx.doi.org/10.1128/aac.00778-15.

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ABSTRACT8-Nitro-benzothiazinones (BTZs), such as BTZ043 and PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity againstMycobacterium tuberculosisin vitro. Structure-activity relationship (SAR) studies revealed the 8-nitro group of the BTZ scaffold to be crucial for the mechanism of action, which involves formation of a semimercaptal bond with Cys387 in the active site of DprE1. To date, substitution of the 8-nitro group has led to extensive loss of antimycobacterial activity. Here, we report the synthesis and characterization of the p
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Warrier, Thulasi, Kanishk Kapilashrami, Argyrides Argyrou, et al. "N-methylation of a bactericidal compound as a resistance mechanism inMycobacterium tuberculosis." Proceedings of the National Academy of Sciences 113, no. 31 (2016): E4523—E4530. http://dx.doi.org/10.1073/pnas.1606590113.

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The rising incidence of antimicrobial resistance (AMR) makes it imperative to understand the underlying mechanisms.Mycobacterium tuberculosis(Mtb) is the single leading cause of death from a bacterial pathogen and estimated to be the leading cause of death from AMR. A pyrido-benzimidazole, 14, was reported to have potent bactericidal activity against Mtb. Here, we isolated multiple Mtb clones resistant to 14. Each had mutations in the putative DNA-binding and dimerization domains ofrv2887, a gene encoding a transcriptional repressor of the MarR family. The mutations in Rv2887 led to markedly i
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Kumar, Avinash, Revathi Rajappan, Suvarna G. Kini, Ekta Rathi, Sriram Dharmarajan, and K. Sreedhara Ranganath Pai. "e-Pharmacophore model-guided design of potential DprE1 inhibitors: synthesis, in vitro antitubercular assay and molecular modelling studies." Chemical Papers 75, no. 10 (2021): 5571–85. http://dx.doi.org/10.1007/s11696-021-01743-3.

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AbstractTuberculosis continues to wreak havoc worldwide and caused around 1.4 million deaths in 2019. Hence, in our pursuit of developing novel antitubercular compounds, we are reporting the e-Pharmacophore-based design of DprE1 (decaprenylphosphoryl-ribose 2′-oxidase) inhibitors. In the present work, we have developed a four-feature e-Pharmacophore model based on the receptor–ligand cavity of DprE1 protein (PDB ID 4P8C) and mapped our previous reported library of compounds against it. The compounds were ranked on phase screen score, and the insights obtained from their alignment were used to
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Zhang, Gang, Song Guo, Huaqing Cui, and Jianguo Qi. "Virtual Screening of Small Molecular Inhibitors against DprE1." Molecules 23, no. 3 (2018): 524. http://dx.doi.org/10.3390/molecules23030524.

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Imran, Mohd, Alshrari A.S., Hamdy Kh Thabet, Abida, and Md Afroz Bakht. "Synthetic molecules as DprE1 inhibitors: A patent review." Expert Opinion on Therapeutic Patents 31, no. 8 (2021): 759–72. http://dx.doi.org/10.1080/13543776.2021.1902990.

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7

R, Manjunatha M., Radha Shandil, Manoranjan Panda, et al. "Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity." ACS Medicinal Chemistry Letters 10, no. 10 (2019): 1480–85. http://dx.doi.org/10.1021/acsmedchemlett.9b00343.

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8

Piton, Jérémie, Caroline S. Y. Foo, and Stewart T. Cole. "Structural studies of Mycobacterium tuberculosis DprE1 interacting with its inhibitors." Drug Discovery Today 22, no. 3 (2017): 526–33. http://dx.doi.org/10.1016/j.drudis.2016.09.014.

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9

Batt, S. M., T. Jabeen, V. Bhowruth, et al. "Structural basis of inhibition of Mycobacterium tuberculosis DprE1 by benzothiazinone inhibitors." Proceedings of the National Academy of Sciences 109, no. 28 (2012): 11354–59. http://dx.doi.org/10.1073/pnas.1205735109.

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10

Chhabra, Sonali, Sunil Kumar, and Raman Parkesh. "Chemical Space Exploration of DprE1 Inhibitors Using Chemoinformatics and Artificial Intelligence." ACS Omega 6, no. 22 (2021): 14430–41. http://dx.doi.org/10.1021/acsomega.1c01314.

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Dissertations / Theses on the topic "DprE1 inhibitors"

1

Chikhale, R., S. Menghani, R. Babu, et al. "Development of selective DprE1 inhibitors: Design, synthesis, crystal structure and antitubercular activity of benzothiazolylpyrimidine-5-carboxamides." 2015. http://hdl.handle.net/10454/7338.

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No<br>Decaprenylphosphoryl-b-d-ribose 20-epimerase (DprE1) is a potential drug target for development of antitubercular agents. Structure based drug discovery approach yielded twenty novel derivatives of benzothiazolylpyrimidine-5-carboxamides (7a–t) which were synthesised by three component one pot reaction involving benzothiazolyl oxobutanamide, thiourea and substituted aromatic benzaldehydes. These derivatives were evaluated for antitubercular activity to determine MIC and compound 7a, 7e, 7f and 7o were found to be potentially active against Mycobacterium tuberculosis (H37Rv). Log P of the
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