Abstract
The discovery and initial optimization of a novel anthranilic acid derived class of antibacterial agents has been described in a recent series of papers. This paper describes the discovery of 1-acylindazol-3-ols as a novel bioisostere of an anthranilic acid. The synthesis and structure-activity relationships of the indazol bioisosteres are described herein.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Combinatorial Chemistry Techniques
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Crystallography, X-Ray
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Indazoles / chemical synthesis*
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Indazoles / chemistry
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Indazoles / pharmacology*
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Microbial Sensitivity Tests
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Molecular Conformation
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Molecular Structure
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Protein Biosynthesis / drug effects*
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Staphylococcus aureus / drug effects*
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Structure-Activity Relationship
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ortho-Aminobenzoates / chemistry*
Substances
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Anti-Bacterial Agents
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Indazoles
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ortho-Aminobenzoates