Design and Synthesis of Heterocyclic Hydroxamic Acid Derivatives as Inhibitors of Helicobacter pylori Urease
Document Type
Article
Publication Date
2003
Publication Source
Synthetic Communications
Abstract
Helicobacter pylori produces ammonia to help counter the acidic environment in the human stomach. The production of ammonia, essential for the microorganism's survival and virulence, is the product of enzymatic conversion of urea by the H. pylori's urease. Inhibition of urease activity by dipeptide hydroxamic acids has previously been demonstrated using a variety of fluorides, thiols and hydroxamic acids. Studies employing computer-aided drug design techniques have been utilized to suggest a novel series of heterocyclic hydroxamic acid derivatives as potential as urease inhibitors. The heterocyclic compounds 7a,b, 10b, 12b, 16b, and 19b have been designed, synthesized, and preliminarily tested as dipeptide mimics which offer a structure that is more biologically stable than that of the reported dipeptide inhibitors.
Inclusive pages
1977-1995
ISBN/ISSN
0039-7911
Copyright
Copyright © 2003, Informa UK
Publisher
Taylor & Francis
Volume
33
Issue
12
Peer Reviewed
yes
eCommons Citation
Muri, Estela M.F.; Mishra, Hetal; Avery, Mitchell A.; and Williamson, John S., "Design and Synthesis of Heterocyclic Hydroxamic Acid Derivatives as Inhibitors of Helicobacter pylori Urease" (2003). Office for Research Publications and Presentations. 22.
https://ecommons.udayton.edu/ofr_pub/22
COinS
Comments
Permission documentation is on file.