1-(1-Arylethylpiperidin-4-yl)thymine Analogs as Antimycobacterial TMPK Inhibitors

Jian, Yanlin; Hulpia, Fabian; Risseeuw, Martijn; Forbes, Harriet; Caljon, Guy; Munier‐Lehmann, Hélène; Boshoff, Helena I.; Calenbergh, Serge Van

doi:10.3390/molecules25122805

Cited by 5 publications

(2 citation statements)

References 34 publications

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“…Currently, TMK inhibitors are mainly evaluated for their use against Mycobacterium tuberculosis infections (Jian et al . 2019 , 2020 ; Venugopala et al . 2020 ).…”

Section: Introductionmentioning

confidence: 99%

The search for novel treatment strategies forStreptococcus pneumoniaeinfections

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Cos

2021

FEMS Microbiology Reviews

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This review provides an overview of the most important novel treatment strategies against Streptococcus pneumoniae infections published over the past 10 years. The pneumococcus causes the majority of community-acquired bacterial pneumonia cases, and it is one of the prime pathogens in bacterial meningitis. Over the last 10 years, extensive research has been conducted to prevent severe pneumococcal infections, with a major focus on (i) boosting the host immune system and (ii) discovering novel antibacterials. Boosting the immune system can be done in two ways, either by actively modulating host immunity, mostly through administration of selective antibodies, or by interfering with pneumococcal virulence factors, thereby supporting the host immune system to effectively overcome an infection. While several of such experimental therapies are promising, few have evolved to clinical trials. The discovery of novel antibacterials is hampered by the high research and development costs versus the relatively low revenues for the pharmaceutical industry. Nevertheless, novel enzymatic assays and target-based drug design, allow the identification of targets and the development of novel molecules to effectively treat this life-threatening pathogen.

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“…Currently, TMK inhibitors are mainly evaluated for their use against Mycobacterium tuberculosis infections (Jian et al . 2019 , 2020 ; Venugopala et al . 2020 ).…”

Section: Introductionmentioning

confidence: 99%

The search for novel treatment strategies forStreptococcus pneumoniaeinfections

Cools

Delputte

Cos

2021

FEMS Microbiology Reviews

View full text Add to dashboard Cite

show abstract

“…Importance was given to the development of an inhibitor of Mycobacterium tuberculosis TMPK (MtbTMPK) which is still belong to the ten causes of death worldwide, killing 1.5 million lives in 2018, thereby preceding AIDS. Thus, a series of 1-(1-arylethylpiperidin-4-yl)thymine analogs as Mycobacterium tuberculosis TMPK (MtbTMPK) inhibitors based on a 1-(1-(3-phenoxyphenethyl)piperidin-4-yl)pyrimidine-2,4(1H,3H)-dione were synthesized and evaluated for their capacity to inhibit MtbTMPK catalytic activity and the growth of a virulent M. tuberculosis strain (H37Rv) by Van Calenbergh [15].…”

mentioning

confidence: 99%