ArticleJournal of medicinal chemistry2018
Discovery and Structure-Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2'-Oxidase.
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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Who cites it
19 citing papers in PubMed, 35 citations in OpenAlex.
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- Identification of a Series Containing a Pentafluorophenyl Moiety That Targets Pks13 to Inhibit Growth ofACS infectious diseases · 2025Article
- Review
- In Silico Development of Novel Benzofuran-1,3,4-Oxadiazoles as Lead Inhibitors ofPharmaceuticals (Basel, Switzerland) · 2023Article
- Synthesis of Novel Benzenesulfonamide-Bearing Functionalized Imidazole Derivatives as Novel Candidates Targeting Multidrug-ResistantMicroorganisms · 2023Article
- Recent Advances of DprE1 Inhibitors againstACS omega · 2022Review
- Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs.Nature communications · 2022Article
- Identification of hydantoin based Decaprenylphosphoryl-β-D-Ribose Oxidase (DprE1) inhibitors as antimycobacterial agents using computational tools.Scientific reports · 2022Article
- Identification of β-Lactams Active againstACS infectious diseases · 2022Article
- Synthesis of 5-unsubstituted dihydropyrimidinone-4-carboxylates from deep eutectic mixtures.Beilstein journal of organic chemistry · 2022Article
- 6-Fluorophenylbenzohydrazides inhibit Mycobacterium tuberculosis growth through alteration of tryptophan biosynthesis.European journal of medicinal chemistry · 2021Article
- 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis inJournal of medicinal chemistry · 2021Article
- Structure-Activity Relationships of Pyrazolo[1,5-ACS infectious diseases · 2021Article
- Tuberculosis Drug Discovery: A Decade of Hit Assessment for Defined Targets.Frontiers in cellular and infection microbiology · 2021Review
- Molecule Property Analyses of Active Compounds forJournal of medicinal chemistry · 2020Review
- Biological Profiling Enables Rapid Mechanistic Classification of Phenotypic Screening Hits and Identification of KatG Activation-Dependent Pyridine Carboxamide Prodrugs With Activity AgainstFrontiers in cellular and infection microbiology · 2020Article
- Inhibition of CorA-Dependent Magnesium Homeostasis Is Cidal in Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 2019Article
Corrections and comments
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Authors and funding
17 authors at 3 institutions in 2 countries.
Funding
Abstract
Magnesium plays an important role in infection with Mycobacterium tuberculosis ( Mtb) as a signal of the extracellular environment, as a cofactor for many enzymes, and as a structural element in important macromolecules. Raltegravir, an antiretroviral drug that inhibits HIV-1 integrase is known to derive its potency from selective sequestration of active-site magnesium ions in addition to binding to a hydrophobic pocket. In order to determine if essential Mtb-related phosphoryl transfers could be disrupted in a similar manner, a directed screen of known molecules with integrase inhibitor-like pharmacophores ( N-alkyl-5-hydroxypyrimidinone carboxamides) was performed. Initial hits afforded compounds with low-micromolar potency against Mtb, acceptable cytotoxicity and PK characteristics, and robust SAR. Elucidation of the target of these compounds revealed that they lacked magnesium dependence and instead disappointingly inhibited a known promiscuous target in Mtb, decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1, Rv3790).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.