萘并[1,2-d]噁唑合成及其衍生物之生物活性評估

本研究主題為探討具備三環共平面的萘并[1,2-d]噁唑衍伸物之合成方法，以及其對於抗發炎的生物活性評估。在萘并[1,2-d]噁唑結構C-2和C-5的修飾上，關於抗發炎活性也已經被我們探索，並且初步確立對於結構活性的關係。在大部分萘并[1,2-d]噁唑衍伸物中，化合物(27a)是最具活性對抗脂多醣(LPS)誘導一氧化氮(NO)產生。在濃度10 μM下化合物(27a)能夠抑制LPS誘導NO產生,而更進一步的結構優化也持續地進行中。

關鍵字

合成；噁唑；抗發炎生物活性

並列摘要

This thesis describes preparation and anti-inflammatory evaluation of certain naphtho[1,2-d]oxazole derivatives which possess the three-ring coplanar pharmacophore. The anti-inflammatory activities with respect to the structural modification on C-2 and C-5 of the naphtho[1,2-d]oxazole pharmacophore have been explored and the preliminary structure-activity relationships have been established. Among these naphtho[1,2-d]oxazole derivatives, compound 27a is the most active against lipopolysaccharide (LPS) induced NO production. Compound 27a is capable of inhibiting LPS-induced NO production completely at a concentration of 10 μM. Further structural optimization is on-going.

並列關鍵字

oxazole ； synthesis ； anti-inflammatory

參考文獻

1. Gordon, S. Nat. Rev. Immuno.2003,3,23-35.

Google Scholar

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