Title: Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents
Authors: Song, Lijun ×
Risseeuw, Martijn D P
Froeyen, Mathy
Karalic, Izet
Goeman, Jan
Cappoen, Davie
Van der Eycken, Johan
Cos, Paul
Munier-Lehmann, Hélène
Van Calenbergh, Serge #
Issue Date: Aug-2016
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:Ahead of print
Article number: S0968-0896(16)30649-6
Abstract: We report the design and synthesis of a series of non-nucleoside MtbTMPK inhibitors (1-14) based on the gram-positive bacterial TMPK inhibitor hit compound 1. A practical synthesis was developed to access these analogues. Several compounds show promising MtbTMPK inhibitory potency and allow the establishment of a structure-activity relationship, which is helpful for further optimization.
ISSN: 0968-0896
Publication status: accepted
KU Leuven publication type: IT
Appears in Collections:Early Modern History (15th-18th Centuries), Leuven
Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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