1999 Fiscal Year Final Research Report Summary
Developmental study of novel anti-ulcerous drug with inhibitory activity of HィイD1+ィエD1, KィイD1+ィエD1-ATPase and preventive action of growth of Helicobactor pylori in gastral cavity
| Project/Area Number |
09672180
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Research Field |
Chemical pharmacy
|
|---|
| Research Institution | Tokushima Bunri University |
|---|
Principal Investigator |
SATOH Toshio Tokushima Bunri University, Professor, 薬学部, 教授 (70075943)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
NISHIKI Mayumi Tokushima Bunri University, Research associate, 薬学部, 助手 (40140610)
MIYATAKA hideki Tokushima Bunri University, Research associate, 薬学部, 助手 (50157658)
MATSUMOTO Hitoshi Tokushima Bunri University, Associate Professor, 薬学部, 助教授 (30109730)
|
|---|
| Project Period (FY) |
1997 – 1999
|
| Keywords | Antiulcer / Antiurease / Allene carboxylate derivatives / Helicobactor pylori / Eradication |
|---|
| Research Abstract |
We have taken notice of the point of view that both proton pump enzyme and the urease of H.pyroli are SH enzyme, and designed and synthesized trisubstituted allencarboxylate derivatives and also investigated antiulcerous and urease inhibitory activities.
From the studies in 1997 and 1998, it was found that chemical shifts of the center carbon shifted to lower, the stronger the biological activities in both antiulcelous and urease inhibitory actions. In 1999, from the results descried above, trisubstituted allencarboxylates with various kinds of functional groups on the aromatic nuclrei, were synthesized and also optically active allencarboxylates were synthesized as well. The physiological activities and reactivity of these compounds with SH compounds and SH enzymes were investigated.
As the results, it was found that introduction of the electron drawing substituentes on the aromatic nuclrei of allenderivatives enforced the inhibitory actions toward SH enzymes. And also founded S type optically active allen-derivatives showed more stronger inhibitory activities to SH enzymes.
The reactivity of the allen derivatives with SH enzymes presumed to be caused by radical dependent reaction in presence of active oxygen.
From these results, trisubstituted allencarboxylate are supposed to be important leading compounds of various kinds of medicines.
|
