MEDI 323 |
| Due to intensive and constant exposure of antibiotics to bacteria, the spread of antibiotic-resistant bacteria occurs much more rapidly in hospitals than in the outside community. An approximate 10% patients requiring long and frequent hospital stay due to surgery or organ replacement or due to opportunistic diseases, are vulnerable to developing resistance even to antibiotic of last resort such as Vancomycin, compared with normal population and lead 1% of this population to death. Successful introduction of a combination therapy of clavulanate, a -lactamase inhibitor and amoxicillin antibiotic for the treatment of infections caused by gram-positive cocci prompted us to investigate a new approach involving the shutting off the enzymes which are responsible for resistance and thus reinstating Vancomycin antibiotic sensitivity. The Vancomycin resistant enterococci (VRE) are characterized by the presence of a zinc binding dipeptidase, namely VanX that removes the cell wall precursor molecule DAla-DAla peptide which is essential for the cell wall synthesis of Vancomycin sensitivite bacteria. Preliminary studies on the synthesis of novel class of VanX inhibitors derived from molecular modeling and enzyme assay suitable for high throughput screening will be presented. |
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Medicinal Chemistry of Rare Diseases
1:30 PM-5:00 PM, Wednesday, 13 September 2006 Moscone Center -- Room 103, Oral
Division of Medicinal Chemistry |