Abstract
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).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemical synthesis
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Amides / pharmacology*
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Amides / toxicity
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Antifungal Agents / chemical synthesis
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Antifungal Agents / pharmacology*
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Antifungal Agents / toxicity
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Chlamydia trachomatis / drug effects*
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Chlamydia trachomatis / pathogenicity
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HeLa Cells
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Humans
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Mutagenicity Tests
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Pyridones / chemical synthesis
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Pyridones / pharmacology*
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Pyridones / toxicity
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Thiazoles / chemical synthesis
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Thiazoles / pharmacology*
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Thiazoles / toxicity
Substances
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Amides
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Antifungal Agents
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Pyridones
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Thiazoles