Abstract
Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and PRSP. 3,4-Difluorophenyl 5-cyanothiazolylurea (3p) with clog P of 2.64 demonstrated antibacterial activity against both gram-positive and gram-negative bacteria.
MeSH terms
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Anti-Bacterial Agents / pharmacology*
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Carbamates / chemistry*
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Carbamates / pharmacology*
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Cell Wall / drug effects
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Cell Wall / enzymology
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Enterococcus faecalis / drug effects
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Enterococcus faecalis / enzymology
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Escherichia coli / drug effects
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Escherichia coli / enzymology
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Microbial Sensitivity Tests
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Peptidoglycan / biosynthesis*
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Phenylthiazolylthiourea / analogs & derivatives*
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Phenylthiazolylthiourea / pharmacology*
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Staphylococcus / drug effects
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Staphylococcus / enzymology
Substances
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Anti-Bacterial Agents
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Carbamates
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Peptidoglycan
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Phenylthiazolylthiourea