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© Research
Publication : European journal of medicinal chemistry

Synthesis and structure activity relationships of cyanopyridone based anti-tuberculosis agents.

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in European journal of medicinal chemistry - 01 Sep 2020

Jian Y, Hulpia F, Risseeuw MDP, Forbes HE, Munier-Lehmann H, Caljon G, Boshoff HIM, Van Calenbergh S,

Link to Pubmed [PMID] – 32623208

Link to DOI [DOI] – S0223-5234(20)30421-910.1016/j.ejmech.2020.112450

Eur J Med Chem 2020 Sep; 201(): 112450

Mycobacterium tuberculosis, the causative agent of tuberculosis, relies on thymidylate kinase (MtbTMPK) for the synthesis of thymidine triphosphates and thus also DNA synthesis. Therefore, this enzyme constitutes a potential Achilles heel of the pathogen. Based on a previously reported MtbTMPK 6-aryl-substituted pyridone inhibitor and guided by two co-crystal structures of MtbTMPK with pyridone- and thymine-based inhibitors, we report the synthesis of a series of aryl-shifted cyanopyridone analogues. These compounds generally lacked significant MtbTMPK inhibitory potency, but some analogues did exhibit promising antitubercular activity. Analogue 11i demonstrated a 10-fold increased antitubercular activity (MIC H37Rv, 1.2 μM) compared to literature compound 5. Many analogues with whole-cell antimycobacterial activity were devoid of significant cytotoxicity.

https://pubmed.ncbi.nlm.nih.gov/32623208