Abstract
| Language | English |
|---|---|
| Pages | 423-439 |
| Number of pages | 17 |
| Journal | BioMetals |
| Volume | 30 |
| Issue number | 3 |
| Early online date | 19 Apr 2017 |
| DOIs | |
| Publication status | Published - 30 Jun 2017 |
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Keywords
- inflammatory bowel disease
- metal-Schiff base
- colitis
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Schiff base complexes of copper and zinc as potential anti-colitic compounds. / Conner, Elaine M.; Reglinski, John; Smith, W. Ewen; Zeitlin, I. Jack.
In: BioMetals, Vol. 30, No. 3, 30.06.2017, p. 423-439.Research output: Contribution to journal › Article
TY - JOUR
T1 - Schiff base complexes of copper and zinc as potential anti-colitic compounds
AU - Conner, Elaine M.
AU - Reglinski, John
AU - Smith, W. Ewen
AU - Zeitlin, I. Jack
PY - 2017/6/30
Y1 - 2017/6/30
N2 - The design, synthesis and activity of polymodal compounds for the treatment of inflammatory bowel disease are reported. The compounds, being based on a metal-Schiff base motif, are designed to degrade during intestinal transit to release the bioactive components in the gut. The compounds have been developed sequential with the biomodal compounds combining copper or zinc with a salicylaldehyde adduct. These compounds were tested in a formalin induced colonic inflammation model in BK:A mice. From these studies a trimodal compound based on a zinc Schiff base analogue of Sulfosalazine were designed. This was tested against a trinitrobenzenesulfonic acid (TNB) induced colitic model in Wistar rats. The use of two models allows us to test our compounds in both an acute and a chronic model. The trimodal compound reported is observed to provide anticolitic properties in the chronic TNB induced colitis model commensurate with that of SASP. However, the design of trimodal compound still has the capacity for further development. This the platform reported may offer a route into compounds which can markedly outperform the anti-colitic properties of SASP.
AB - The design, synthesis and activity of polymodal compounds for the treatment of inflammatory bowel disease are reported. The compounds, being based on a metal-Schiff base motif, are designed to degrade during intestinal transit to release the bioactive components in the gut. The compounds have been developed sequential with the biomodal compounds combining copper or zinc with a salicylaldehyde adduct. These compounds were tested in a formalin induced colonic inflammation model in BK:A mice. From these studies a trimodal compound based on a zinc Schiff base analogue of Sulfosalazine were designed. This was tested against a trinitrobenzenesulfonic acid (TNB) induced colitic model in Wistar rats. The use of two models allows us to test our compounds in both an acute and a chronic model. The trimodal compound reported is observed to provide anticolitic properties in the chronic TNB induced colitis model commensurate with that of SASP. However, the design of trimodal compound still has the capacity for further development. This the platform reported may offer a route into compounds which can markedly outperform the anti-colitic properties of SASP.
KW - inflammatory bowel disease
KW - metal-Schiff base
KW - colitis
UR - https://link.springer.com/journal/volumesAndIssues/10534
U2 - 10.1007/s10534-017-0016-z
DO - 10.1007/s10534-017-0016-z
M3 - Article
VL - 30
SP - 423
EP - 439
JO - BioMetals
T2 - BioMetals
JF - BioMetals
SN - 0966-0844
IS - 3
ER -