發明
中華民國
103112492
I 510474
抑制莽草酸路徑之化合物及其用途
國立清華大學
2015/12/01
幽門螺旋桿菌(H.pylori)是一種微好氣性的螺旋狀或彎曲狀 的革蘭氏陰性菌,棲息在人類胃黏膜,世界各地有超過50%人口感染幽門螺旋桿菌,長期感染幽門螺旋桿菌可能會造成胃炎,進而發展成胃潰瘍,萎縮性胃炎,甚至胃癌,隨著傳統抗生素已漸漸因為抗藥性問題而療效不彰,發展新型的抗生素成為重要課題。莽草酸代謝路徑是合成芳香族胺基酸的重要上游途徑,而且只存在於微生物、植物及寄生蟲當中,而不存在於哺乳動物,遂成為發展抗生素的良好標的。本發明提供一種製備方法及抑制莽草酸代謝路徑之化合物,本發明還提供一種具有協同抗菌化合物組合物。 Helicobacter pylori (H. pylori) are microaerophilic gram-negative bacteria which inhabits the gastric mucosa of humans. Enduring infection by H. pylori provokes active gastritis, alters gastric physiology, and may subsequently lead to peptic ulcer, atrophic gastritis, or even gastric adenocarcinoma. H. pylori can be eradicated by the standard triple therapy. The treatment of H. pylori infection using high-dosage antibiotics, however, has resulted in drug resistance. The need for new antibacterial therapies is therefore a major concern of healthcare professionals. The shikimate pathway is unique to microbial cells and parasites but absent in animals. Therefore, enzymes of this pathway are attractive targets for the development of nontoxic antimicrobial compounds. The present invention provides methods and compounds of inhibiting shikimate pathway in a non-mammal host. The present invention also provides a synergistic antibacterial composition.
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