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Journal articles on the topic 'DprE1 inhibitors'

Author: Grafiati

Published: 4 June 2021

Last updated: 18 February 2022

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1

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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2

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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3

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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4

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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5

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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6

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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11

Yalcin, Gozde, Serdar Burmaoglu, Ilkay Yildiz, and Oztekin Algul. "Molecular docking studies on fluoro-substituted chalcones as potential DprE1 enzyme inhibitors." Journal of Molecular Structure 1164 (July 2018): 50–56. http://dx.doi.org/10.1016/j.molstruc.2018.02.087.

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12

Liu, Lingfeng, Chengcheng Kong, Marco Fumagalli, et al. "Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents." European Journal of Medicinal Chemistry 208 (December 2020): 112773. http://dx.doi.org/10.1016/j.ejmech.2020.112773.

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13

Degiacomi, Giulia, Juan Manuel Belardinelli, Maria Rosalia Pasca, Edda De Rossi, Giovanna Riccardi, and Laurent Roberto Chiarelli. "Promiscuous Targets for Antitubercular Drug Discovery: The Paradigm of DprE1 and MmpL3." Applied Sciences 10, no. 2 (2020): 623. http://dx.doi.org/10.3390/app10020623.

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The development and spread of Mycobacterium tuberculosis multi-drug resistant strains still represent a great global health threat, leading to an urgent need for novel anti-tuberculosis drugs. Indeed, in the last years, several efforts have been made in this direction, through a number of high-throughput screenings campaigns, which allowed for the identification of numerous hit compounds and novel targets. Interestingly, several independent screening assays identified the same proteins as the target of different compounds, and for this reason, they were named “promiscuous” targets. These prote

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14

Balabon, Olga, Eleni Pitta, Maciej K. Rogacki та ін. "Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors". Journal of Medicinal Chemistry 63, № 10 (2020): 5367–86. http://dx.doi.org/10.1021/acs.jmedchem.0c00107.

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15

Chikhale, Rupesh V., Mahesh A. Barmade, Prashant R. Murumkar, and Mange Ram Yadav. "Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis." Journal of Medicinal Chemistry 61, no. 19 (2018): 8563–93. http://dx.doi.org/10.1021/acs.jmedchem.8b00281.

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16

Niranjan Kumar, Rakesh Srivastava, Amresh Prakash, and Andrew M. Lynn. "Virtual screening and free energy estimation for identifying Mycobacterium tuberculosis flavoenzyme DprE1 inhibitors." Journal of Molecular Graphics and Modelling 102 (January 2021): 107770. http://dx.doi.org/10.1016/j.jmgm.2020.107770.

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17

Rogacki, Maciej K., Eleni Pitta, Olga Balabon, et al. "Identification and Profiling of Hydantoins—A Novel Class of Potent Antimycobacterial DprE1 Inhibitors." Journal of Medicinal Chemistry 61, no. 24 (2018): 11221–49. http://dx.doi.org/10.1021/acs.jmedchem.8b01356.

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18

Trefzer, Claudia, Henrieta Škovierová, Silvia Buroni та ін. "Benzothiazinones Are Suicide Inhibitors of Mycobacterial Decaprenylphosphoryl-β-d-ribofuranose 2′-Oxidase DprE1". Journal of the American Chemical Society 134, № 2 (2011): 912–15. http://dx.doi.org/10.1021/ja211042r.

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19

Wang, Pengxu, Sarah M. Batt, Bin Wang, et al. "Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities." Journal of Medicinal Chemistry 64, no. 9 (2021): 6241–61. http://dx.doi.org/10.1021/acs.jmedchem.1c00263.

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20

Verma, H., S. Choudhary, M. Kumar, and O. Silakari. "In silico guided design of non-covalent inhibitors of DprE1: synthesis and biological evaluation." SAR and QSAR in Environmental Research 32, no. 4 (2021): 333–52. http://dx.doi.org/10.1080/1062936x.2021.1900390.

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21

Shirude, Pravin S., Radha Shandil, Claire Sadler, et al. "Azaindoles: Noncovalent DprE1 Inhibitors from Scaffold Morphing Efforts, Kill Mycobacterium tuberculosis and Are Efficaciousin Vivo." Journal of Medicinal Chemistry 56, no. 23 (2013): 9701–8. http://dx.doi.org/10.1021/jm401382v.

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22

Saxena, Anil Kumar, and Anamika Singh. "Mycobacterial tuberculosis Enzyme Targets and their Inhibitors." Current Topics in Medicinal Chemistry 19, no. 5 (2019): 337–55. http://dx.doi.org/10.2174/1568026619666190219105722.

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Tuberculosis (TB) still continues to be a major killer disease worldwide. Unlike other bacteria Mycobacterium tuberculosis (Mtb) has the ability to become dormant within the host and to develop resistance. Hence efforts are being made to overcome these problems by searching for new antitubercular agents which may be useful in the treatment of multidrug-(MDR) and extensively drugresistant (XDR) M. tuberculosis and shortening the treatment time. The recent introduction of bedaquiline to treat MDR-TB and XDR-TB may improve the status of TB treatment. The target enzymes in anti-TB drug discovery p

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23

KB, Suma, Ankita Kumari, Diya Shetty, et al. "Structure based pharmacophore modelling approach for the design of azaindole derivatives as DprE1 inhibitors for tuberculosis." Journal of Molecular Graphics and Modelling 101 (December 2020): 107718. http://dx.doi.org/10.1016/j.jmgm.2020.107718.

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24

Naik, Maruti, Vaishali Humnabadkar, Subramanyam J. Tantry, et al. "4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity." Journal of Medicinal Chemistry 57, no. 12 (2014): 5419–34. http://dx.doi.org/10.1021/jm5005978.

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25

Chikhale, Rupesh, Sunil Menghani, Ramavath Babu, et al. "Development of selective DprE1 inhibitors: Design, synthesis, crystal structure and antitubercular activity of benzothiazolylpyrimidine-5-carboxamides." European Journal of Medicinal Chemistry 96 (May 2015): 30–46. http://dx.doi.org/10.1016/j.ejmech.2015.04.011.

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26

Ravi, Bentham Science Publisher, and S. K. Mahmood. "Pharmacophore Modeling, 3DQSAR and Structural Analysis of new Class of Potent Antimycobacterial Agents1, 3-Benzothiazin-4-Onescompounds as DprE1 Inhibitors." Letters in Drug Design & Discovery 12, no. 999 (2014): 1. http://dx.doi.org/10.2174/1570180812666141201222756.

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27

Kumar, Avinash, Revathi Rajappan, Suvarna G. Kini, Ekta Rathi, Sriram Dharmarajan, and K. Sreedhara Ranganath Pai. "Correction to: e-Pharmacophore model-guided design of potential DprE1 inhibitors: synthesis, in vitro antitubercular assay and molecular modelling studies." Chemical Papers 75, no. 11 (2021): 6145. http://dx.doi.org/10.1007/s11696-021-01762-0.

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28

Mariandyshev, A. O., A. L. Khokhlov, S. V. Smerdin, et al. "The main results of clinical trials of the efficacy, safety and pharmacokinetics of the perspective anti-tuberculosis drug makozinone (PBTZ169)." Terapevticheskii arkhiv 92, no. 3 (2020): 61–72. http://dx.doi.org/10.26442/00403660.2020.03.000621.

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Tuberculosis is a chronic infectious disease, usually localized in the respiratory system and representing one of the most important global social and biomedical health problems associated with the spread of therapy-resistant forms (multidrug-resistant and extensively drug-resistant tuberculosis). One of the most promising targets for the development of antimycobacterial drugs is the enzyme DprE1, which is involved in the synthesis of the cell wall of mycobacteria. In the series of DprE1 inhibitor drugs, the most advanced drug is PBTZ169 (INN maсozinone). Clinical trials (CT) of the efficacy a

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29

Goldman, Robert C. "Target Discovery for New Antitubercular Drugs Using a Large Dataset of Growth Inhibitors from PubChem." Infectious Disorders - Drug Targets 20, no. 3 (2020): 352–66. http://dx.doi.org/10.2174/1871526519666181205163810.

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The number of drugs available for treatment of active tuberculosis is diminishing due to increased multidrug resistance selection in Mycobacterium tuberculosis leading to multiple (MDR) and extensively (XDR) resistant strains. Also, TB is treated with multiple drugs to minimize further resistance development, mandating a sustained effort to identify new lead compounds for treating drug-resistant TB and shortening time to cure for all TB infections. High throughput screening, a well-known approach to discovery of new leads, is conducted in two basic modes 1) using whole cells and screening for

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30

Maharaj, Yushir, Soumendranath Bhakat, and Mahmoud Soliman. "Computer-aided Identification of Novel DprE1 Inhibitors as Potential Anti-TB Lead Compounds: A Hybrid Virtual-screening and Molecular Dynamics Approach." Letters in Drug Design & Discovery 12, no. 4 (2015): 302–13. http://dx.doi.org/10.2174/1570180811666141001005536.

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31

Whitehurst, Benjamin C., Robert J. Young, Glenn A. Burley, Monica Cacho, Pedro Torres, and Laura Vela-Gonzalez del Peral. "Identification of 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-N-phenylpropanamides as a novel class of potent DprE1 inhibitors." Bioorganic & Medicinal Chemistry Letters 30, no. 12 (2020): 127192. http://dx.doi.org/10.1016/j.bmcl.2020.127192.

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32

Gawad, Jineetkumar, and Chandrakant Bonde. "Design, synthesis and biological evaluation of novel 6-(trifluoromethyl)-N-(4-oxothiazolidin-3-yl)quinazoline-2-carboxamide derivatives as a potential DprE1 inhibitors." Journal of Molecular Structure 1217 (October 2020): 128394. http://dx.doi.org/10.1016/j.molstruc.2020.128394.

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33

Dey, Rishita, Sisir Nandi, Asmita Samadder, Aaruni Saxena, and Anil Kumar Saxena. "Exploring the Potential Inhibition of Candidate Drug Molecules for Clinical Investigation Based on their Docking or Crystallographic Analyses against M. tuberculosis Enzyme Targets." Current Topics in Medicinal Chemistry 20, no. 29 (2020): 2662–80. http://dx.doi.org/10.2174/1568026620666200903163921.

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Tuberculosis (TB) is a devastating disease responsible for millions of humans’ deaths worldwide. It is caused by a mycobacterial organism, the tubercle bacillus or Mycobacterium tuberculosis. Although TB can be treated, cured and can be prevented if patients take prescribed medicines, scientists have never come close to wiping it out due to a sharp rise in the incidence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) mycobacterium strains. Due to long regimen treatment and emergence of MDR and XDR-TB, it is urgent to re-engineer and reposition old drugs for developing new ant

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34

Verma, Himanshu, Shalki Choudhary, Pankaj Kumar Singh, Aanchal Kashyap, and Om Silakari. "Decoding the signature of molecular mechanism involved in mutation associated resistance to 1, 3-benzothiazin-4-ones (Btzs) based DprE1 inhibitors using BTZ043 as a reference drug." Molecular Simulation 45, no. 18 (2019): 1515–23. http://dx.doi.org/10.1080/08927022.2019.1659507.

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35

Gawad, Jineetkumar, and Chandrakant Bonde. "Design, synthesis and biological evaluation of some 2-(6-nitrobenzo[d]thiazol-2-ylthio)-N-benzyl-N-(6-nitrobenzo[d]thiazol-2-yl)acetamide derivatives as selective DprE1 inhibitors." Synthetic Communications 49, no. 20 (2019): 2696–708. http://dx.doi.org/10.1080/00397911.2019.1639756.

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36

., Santosh L. Kumbhare, Sampatrao B. Suryawanshi ., Vijay H. Masand ., and Suryakant B. Borul . "Consensus Pharmacophore identification for antimycobacterial DprE1 inhibitory activity of substituted hydantoins." Journal of Current Pharma Research 9, no. 2 (2019): 2721–26. http://dx.doi.org/10.33786/jcpr.2019.v09i02.002.

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37

Lechartier, Benoit, Ruben C. Hartkoorn, and Stewart T. Cole. "In VitroCombination Studies of Benzothiazinone Lead Compound BTZ043 against Mycobacterium tuberculosis." Antimicrobial Agents and Chemotherapy 56, no. 11 (2012): 5790–93. http://dx.doi.org/10.1128/aac.01476-12.

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ABSTRACTBenzothiazinones (BTZ) are a new class of drug candidates to combat tuberculosis that inhibit decaprenyl-phosphoribose epimerase (DprE1), an essential enzyme involved in arabinan biosynthesis. Using the checkerboard method and cell viability assays, we have studied the interaction profiles of BTZ043, the current lead compound, with several antituberculosis drugs or drug candidates againstMycobacterium tuberculosisstrain H37Rv, namely, rifampin, isoniazid, ethambutol, TMC207, PA-824, moxifloxacin, meropenem with or without clavulanate, and SQ-109. No antagonism was found between BTZ043

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38

Baptista, Rafael, Sumana Bhowmick, Jianying Shen, and Luis A. J. Mur. "Molecular Docking Suggests the Targets of Anti-Mycobacterial Natural Products." Molecules 26, no. 2 (2021): 475. http://dx.doi.org/10.3390/molecules26020475.

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Tuberculosis (TB) is a major global threat, mostly due to the development of antibiotic-resistant forms of Mycobacterium tuberculosis, the causal agent of the disease. Driven by the pressing need for new anti-mycobacterial agents several natural products (NPs) have been shown to have in vitro activities against M. tuberculosis. The utility of any NP as a drug lead is augmented when the anti-mycobacterial target(s) is unknown. To suggest these, we used a molecular reverse docking approach to predict the interactions of 53 selected anti-mycobacterial NPs against known “druggable” mycobacterial t

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39

Panda, Manoranjan, Sreekanth Ramachandran, Vasanthi Ramachandran, et al. "Discovery of Pyrazolopyridones as a Novel Class of Noncovalent DprE1 Inhibitor with Potent Anti-Mycobacterial Activity." Journal of Medicinal Chemistry 57, no. 11 (2014): 4761–71. http://dx.doi.org/10.1021/jm5002937.

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40

Gao, Ya, Jinshan Xie, Ruotian Tang, et al. "Identification of a pyrimidinetrione derivative as the potent DprE1 inhibitor by structure-based virtual ligand screening." Bioorganic Chemistry 85 (April 2019): 168–78. http://dx.doi.org/10.1016/j.bioorg.2018.12.018.

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41

Bolger, G., T. Michaeli, T. Martins, et al. "A family of human phosphodiesterases homologous to the dunce learning and memory gene product of Drosophila melanogaster are potential targets for antidepressant drugs." Molecular and Cellular Biology 13, no. 10 (1993): 6558–71. http://dx.doi.org/10.1128/mcb.13.10.6558.

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We have isolated cDNAs for four human genes (DPDE1 through DPDE4) closely related to the dnc learning and memory locus of Drosophila melanogaster. The deduced amino acid sequences of the Drosophila and human proteins have considerable homology, extending beyond the putative catalytic region to include two novel, highly conserved, upstream conserved regions (UCR1 and UCR2). The upstream conserved regions are located in the amino-terminal regions of the proteins and appear to be unique to these genes. Polymerase chain reaction analysis suggested that these genes encoded the only homologs of dnc

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42

Bolger, G., T. Michaeli, T. Martins, et al. "A family of human phosphodiesterases homologous to the dunce learning and memory gene product of Drosophila melanogaster are potential targets for antidepressant drugs." Molecular and Cellular Biology 13, no. 10 (1993): 6558–71. http://dx.doi.org/10.1128/mcb.13.10.6558-6571.1993.

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We have isolated cDNAs for four human genes (DPDE1 through DPDE4) closely related to the dnc learning and memory locus of Drosophila melanogaster. The deduced amino acid sequences of the Drosophila and human proteins have considerable homology, extending beyond the putative catalytic region to include two novel, highly conserved, upstream conserved regions (UCR1 and UCR2). The upstream conserved regions are located in the amino-terminal regions of the proteins and appear to be unique to these genes. Polymerase chain reaction analysis suggested that these genes encoded the only homologs of dnc

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43

Xu, Mengmeng, Yanbei Zhang, Muyun Wang, et al. "TRPV1 and TRPA1 in Lung Inflammation and Airway Hyperresponsiveness Induced by Fine Particulate Matter (PM2.5)." Oxidative Medicine and Cellular Longevity 2019 (June 2, 2019): 1–15. http://dx.doi.org/10.1155/2019/7450151.

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Exposure to fine particulate matter (PM2.5) has been associated with lung inflammation and airway hyperresponsiveness (AHR). Transient receptor potential (TRP) vanilloid 1 (TRPV1) and ankyrin 1 (TRPA1) both may play important roles in lung inflammation and AHR. We investigated whether PM2.5-induced lung inflammation and AHR could be prevented by blocking TRPV1 and TRPA1 channels. Mice were injected intraperitoneally with AMG9810 (30 mg/kg, a TRPV1 antagonist) or A967079 (30 mg/kg, a TRPA1 antagonist) or their combination or vehicle (PBS) one hour before intranasal instillation of PM2.5 (7.8 mg

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44

Ganesh, Neenu, Arun Kumar S, Manisha Singh, Venkaraddi Mangannavar Chandrashekar, and Gurubasavaraj Veeranna Pujar. "Antitubercular Potential of Novel Isoxazole Encompassed 1, 2, 4-Triazoles: Design, Synthesis, Molecular Docking Study and Evaluation of Antitubercular Activity." Anti-Infective Agents 18 (July 11, 2020). http://dx.doi.org/10.2174/2211352518999200711163714.

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Background: Decaprenylphosphoryl-β-D-ribose epimerase (DprE1), a flavoprotein enzyme engaged in the biosynthesis of decaprenylphosphoryl-β-D-arabinofuranose (DPA), is the only contributor of arabinose residues which is fundamental for the mycobacterium cell wall constituents. DprE1 is an interesting target for antitubercular agent and has been exploring to develop potential chemical entities as antitubercular agents. Objective: The objective of study is the development of novel antitubercular agents targeting Mtb Decaprenylphosphoryl-βD-ribose epimerase (DprE1). Methods: A series of isoxazole

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45

Robertson, Gregory T., Michelle E. Ramey, Lisa M. Massoudi, et al. "Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 inhibitors TBA-7371, PBTZ169 and OPC-167832." Antimicrobial Agents and Chemotherapy, August 9, 2021. http://dx.doi.org/10.1128/aac.00583-21.

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Multiple drug discovery initiatives for tuberculosis are currently ongoing to identify and develop new potent drugs with novel targets in order to shorten treatment duration. One of the drug classes with a new mode of action are DprE1 inhibitors targeting an essential process in cell wall synthesis of Mycobacterium tuberculosis . In this investigation, three DprE1 inhibitors currently in clinical trials, TBA-7371, PBTZ169 and OPC-167832, were evaluated side-by-side as single agents in the C3HeB/FeJ mouse model presenting with caseous necrotic pulmonary lesions upon tuberculosis infection. The

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46

Piton, Jérémie, Anthony Vocat, Andréanne Lupien, et al. "Structure-Based Drug Design and Characterization of Sulfonyl-Piperazine Benzothiazinone Inhibitors of DprE1 from Mycobacterium tuberculosis." Antimicrobial Agents and Chemotherapy 62, no. 10 (2018). http://dx.doi.org/10.1128/aac.00681-18.

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ABSTRACT Macozinone (MCZ) is a tuberculosis (TB) drug candidate that specifically targets the essential flavoenzyme DprE1, thereby blocking synthesis of the cell wall precursor decaprenyl phosphoarabinose (DPA) and provoking lysis of Mycobacterium tuberculosis. As part of the MCZ backup program, we exploited structure-guided drug design to produce a new series of sulfone-containing derivatives, 2-sulfonylpiperazin 8-nitro 6-trifluoromethyl 1,3-benzothiazin-4-one, or sPBTZ. These compounds are less active than MCZ but have a better solubility profile, and some derivatives display enhanced stabi

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47

Xiong, Lu, Chao Gao, Yao-Jie Shi, et al. "Metabolism of SKLB-TB1001, a Potent Antituberculosis Agent, in Animals." Antimicrobial Agents and Chemotherapy 62, no. 7 (2018). http://dx.doi.org/10.1128/aac.02375-17.

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ABSTRACTTuberculosis is a major global health problem, and the emergence of multidrug-resistant and extensively drug-resistant strains has increased the difficulty of treating this disease. Among the novel antituberculosis drugs in the pipeline, decaprenylphosphoryl-beta-d-ribose-2-epimerase (DprE1) inhibitors such as BTZ043 and pBTZ169 exhibited extraordinary antituberculosis potency. Here, the metabolites of the new DprE1 inhibitor SKLB-TB1001in vivoand its inhibition of cytochrome P450 isoforms and plasma protein binding (PPB)in vitrowere studied. The results showed that rapid transformatio

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Chikhale, Rupesh V., Amit M. Pant, Sunil S. Menghani, and Pramod B. Khedekar. "Development of dual inhibitors targeting DprE1 and AHAS for treatment of Mycobacterium tuberculosis infection." BMC Infectious Diseases 14, S3 (2014). http://dx.doi.org/10.1186/1471-2334-14-s3-e24.

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Bonde, Chandrakant, Jineetkumar Gawad та Smita Bonde. "Insights into development of Decaprenyl-phosphoryl-β-D-ribose 2′-epimerase (DprE1) inhibitors as antitubercular agents: A state of the art review". Indian Journal of Tuberculosis, вересень 2021. http://dx.doi.org/10.1016/j.ijtb.2021.09.003.

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Gawad, Jineetkumar, and Chandrakant Bonde. "Synthesis, biological evaluation and molecular docking studies of 6-(4-nitrophenoxy)-1H-imidazo[4,5-b]pyridine derivatives as novel antitubercular agents: future DprE1 inhibitors." Chemistry Central Journal 12, no. 1 (2018). http://dx.doi.org/10.1186/s13065-018-0515-1.

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