Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

Lijun Song; Martijn D.P. Risseeuw; Matheus Froeyen; Izet Karalic; Jan Goeman; Davie Cappoen; Johan Van Der Eycken; Paul Cos; Hélène Munier-Lehmann; Serge Van Calenbergh; Martijn Risseeuw; Mathy Froeyen

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

Lijun Song ¹ Martijn D.P. Risseeuw ¹ Matheus Froeyen ² Izet Karalic ¹ Jan Goeman ¹ Davie Cappoen ³ Johan Van Der Eycken ¹ Paul Cos ³ Hélène Munier-Lehmann ⁴ Serge Van Calenbergh ^{1, *} Martijn Risseeuw Mathy Froeyen ⁵

* Corresponding author

1 UGENT - Ghent University [Belgium]

2 Rega Institute for Medical Research

3 UA - University of Antwerp

4 Chimie et Biocatalyse

5 KU Leuven - Catholic University of Leuven - Katholieke Universiteit Leuven

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.

Keywords : Inhibitors Mycobacterium tuberculosis Thymidine monophosphate kinase Thymine derivatives XDR-TB extensively drug-resistant tuberculosis

Document type :

Journal articles

Domain :

Chemical Sciences

Life Sciences [q-bio]

Complete list of metadatas

Cited literature [11 references] Display Hide Download

https://hal-pasteur.archives-ouvertes.fr/pasteur-01616045
Contributor : Hélène Munier-Lehmann <>
Submitted on : Friday, October 13, 2017 - 2:57:08 PM
Last modification on : Thursday, February 21, 2019 - 10:31:47 AM
Long-term archiving on : Sunday, January 14, 2018 - 1:32:56 PM

BMC_R1_final.pdf

Files produced by the author(s)

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

File

Identifiers

Collections

Citation

Export

Metrics

142

109

Contact

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

File

Identifiers

Collections

Citation

Export

Share

Metrics

142

109

Contact