Synthesis and Structure-Activity Relationship Studies of Benzo[b][1,4]oxazin-3(4H)-one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X.

Clicks: 176
ID: 275502
2019
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Abstract
Since the discovery of a flavin-dependent thymidylate synthase (ThyX or FDTS) that is absent in humans but crucial for DNA biosynthesis in a diverse group of pathogens, the enzyme has been pursued for the development of new antibacterial agents against Mycobacterium tuberculosis, the causative agent of the widespread infectious disease tuberculosis (TB). In response to a growing need for more effective anti-TB drugs, we have built upon our previous screening efforts and report herein an optimization campaign of a novel series of inhibitors with a unique inhibition profile. The inhibitors display competitive inhibition toward the methylene tetrahydrofolate cofactor of ThyX, enabling us to generate a model of the compounds bound to their target, thus offering insight into their structure-activity relationships.
Reference Key
modranka2019synthesischemmedchem Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Modranka, Jakub;Li, Jiahong;Parchina, Anastasia;Vanmeert, Michiel;Dumbre, Shrinivas;Salman, Mayla;Myllykallio, Hannu;Becker, Hubert F;Vanhoutte, Roeland;Margamuljana, Lia;Nguyen, Hoai;Abu El-Asrar, Rania;Rozenski, Jef;Herdewijn, Piet;De Jonghe, Steven;Lescrinier, Eveline;
Journal ChemMedChem
Year 2019
DOI
10.1002/cmdc.201800739
URL
Keywords
tuberculosis antibiotics drug discovery benzo[b][1,4]oxazine

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