A new series of 1,2,4-trioxanes 9a1-a4, 9b1-b4, 10–13 and 9c1-c4 were synthesized and evaluated against multidrug-resistant Plasmodium yoelii nigeriensis in Swiss mice via oral and intramuscular (i.m.) routes. Adamantane-based trioxane 9b4, the most active compound of the series, provided 100% protection to the infected mice at the dose 48 mg/kg × 4 days and 100% clearance of parasitemia at the dose 24 mg/kg × 4 days via oral route. Adamantane-based trioxane 9b4, is twice active than artemisinin.

We have also studied the photooxygenation behaviour of allylic alcohols 6a-b (3-(4-alkoxynaphthyl)-but-2-ene-1-ols) and 6c (3-[4-(tert-butyl-dimethyl-silanyloxy)-naphthalen-1-yl]-but-2-en-1-ol). Being behaving as dienes, they furnished corresponding endoperoxides, while behaving as allylic alcohols, they yielded β-hydroxyhydroperoxides. All the endoperoxides (7a-c) and β-hydroxyhydroperoxides (8a-c) have been separately elaborated to the corresponding 1,2,4-trioxanes, except from endoperoxide 7c. It is worthy to note that TBDMS protected naphthoyl endoperoxide 7c unable to deliver 1,2,4-trioxane, which demonstrated the strength of the O-Si bond is not easy to cleave under acidic condition.

一系列新的1,2,4-三氧杂环己烷的9A1-A4，9B1-B4 10 - 13和9C1-C4的合成和抗耐多药评价约氏疟原虫nigeriensis通过口服和肌内（在Swiss小鼠IM）途径。以金刚烷为基础的三恶烷9b4是该系列中最活跃的化合物，在 48 mg/kg × 4 天的剂量下为受感染的小鼠提供 100% 的保护，在 24 mg/kg × 4 天的剂量下通过口服提供 100% 的寄生虫血症清除率路线。基于金刚烷的三恶烷9b4 的活性是青蒿素的两倍。

我们还研究了烯丙醇6a - b (3-(4-alkoxynaphthyl)-but-2-ene-1-ols) 和6c (3-[4-( tert -butyl-dimethyl-silanyloxy)-萘-1-基]-丁-2-烯-1-醇）。它们表现为二烯，提供相应的内过氧化物，而表现为烯丙醇，则产生β-羟基氢过氧化物。除内过氧化物7c外，所有内过氧化物 ( 7a-c ) 和 β-羟基氢过氧化物 ( 8a-c ) 已分别详细说明为相应的 1,2,4-三恶烷。值得注意的是，TBDMS 保护了萘甲酰内过氧化物7c无法传递1,2,4-三恶烷，这表明O-Si键的强度在酸性条件下不易断裂。