Abstract
Two well-defined oxidative chlorination-cyclization processes have been developed for the stereoselective synthesis of a variety of 4-amido-isothiazolidinone oxide derivatives. The stereochemistry of the cyclization products was confirmed by X-ray crystallography. These new compounds were designed as bacterial serine protease inhibitors. In tests, some of them showed weak antibacterial activity.
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology
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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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Chlorine / chemistry
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Cyclization
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Enterobacter cloacae / drug effects
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Klebsiella pneumoniae / drug effects
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Microbial Sensitivity Tests
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Molecular Conformation
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Moraxella catarrhalis / drug effects
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology
Substances
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Amides
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Anti-Bacterial Agents
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Thiazoles
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Chlorine