Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 22, Pages 9393-9399Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00716
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Funding
- Swedish Research Council
- Knut and Alice Wallenberg Foundation
- Goran Gustafsson Foundation
- Swedish Foundation for Strategic Research
- JC Kempe Foundation
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Chlamydia trachomatis is a global health burden due to its prevalence as a sexually transmitted disease and as the causative agent of the eye infection trachoma. We recently discovered 3-amido thiazolino 2-pyridones which attenuated C. trachomatis infectivity without affecting host cell or commensal bacteria viability. We present here the synthesis and evaluation of nonhydrolyzable amide isosteres based on this class, leading to highly potent 1,2,3-triazole based infectivity inhibitors (EC50 <= 20 nM).
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