Abstract
The mechanochemical synthesis and characterization of a zinc complex with famotidine is described. The complex was characterized by microanalysis and a number of spectroscopic techniques. The complex was of M:L dihydrate type. Derivatization of famotidine with zinc appears to enhance the activity of the drug by inhibiting the growth of Helicobacter pylori (two reference and 34 clinical isolates). The complex inhibited the growth of H. pylori in an MIC range of 18 μg mL-1. The anti-H. pylori activity of the zinc-famotidine complex against antibiotic-resistant strains was nearly comparable to that of antibiotic-susceptible strains. The complex was found to be far less toxic than the parent drug, as demonstrated by its higher LD 50 value. In the human urease enzyme inhibition assay the complex exhibited significant inhibition. The new complex appears to be more useful in eradicating both the antibiotic-susceptible and antibiotic-resistant strains of H. pylori.
| Original language | English |
|---|---|
| Pages (from-to) | 383-390 |
| Number of pages | 8 |
| Journal | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Volume | 25 |
| Issue number | 3 |
| DOIs | |
| State | Published - 2010 |
| Externally published | Yes |
Bibliographical note
Funding Information:associated with this work. One of the authors (M.A.) is grateful to the Higher Education Commission of Pakistan for providing financial assistance to study at the University of Bristol.
Keywords
- Anti-H. pylori activity
- Antiulcer drugs
- Mechanochemical synthesis
- Metal-based drugs
- Urease inhibition
- Zinc complexes
- Zinc-famotidine
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery