Malaria-infected mice live until at least day 30 after a new artemisinin-derived thioacetal thiocarbonate combined with mefloquine are administered together in a single, low, oral dose.
Malaria-infected mice live until at least day 30 after a new artemisinin-derived thioacetal thiocarbonate combined with mefloquine are administered together in a single, low, oral dose.
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疟疾感染的小鼠直到至少30天才生存，此前将新的阿耳马素衍生的硫代硫苯甲酸硫碳纤维与甲氟喹结合在一起，以一种单一的低口服剂量组合在一起。
DOI：
10.1021/jm3009986
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发表时间：
2012-09-13
影响因子：
7.3
通讯作者：
Posner, Gary H.
中科院分区：
文献类型：
--
作者：
Jacobine, Alexander M.;Mazzone, Jennifer R.;Slack, Rachel D.;Tripathi, Abhai K.;Sullivan, David J.;Posner, Gary H.
以天然三环型青蒿素为原料，仅用三步，总收率为21 - 67%，制备了一系列新的21种三环型C-10硫缩醛。单次口服6毫克/公斤的单体三氧环12c和18毫克/公斤的盐酸甲氟喹，感染伯氏疟原虫的小鼠在感染后平均存活29.8天。该组4只小鼠中有2只在感染后第30天的血液中没有检测到寄生虫，它们的行为正常，看起来很健康。其中1只小鼠在第30天血液寄生虫率为11%，该组1只小鼠在第29天死亡。具有高度药用价值的是，这种ACT化疗的疗效远远优于（几乎两倍）在相同条件下使用常用的三氧环类药物蒿甲醚加盐酸甲氟喹作为阳性对照（平均生存时间仅为16.5天）。
In only three steps and in 21–67% overall yields from the natural trioxane artemisinin, a series of 21 new trioxane C-10 thioacetals was prepared. Upon receiving a single oral dose of only 6 mg/kg of the monomeric trioxane 12c combined with 18 mg/kg of mefloquine hydrochloride, Plasmodium berghei-infected mice survived on average 29.8 days after infection. Two of the four mice in this group had no parasites detectable in their blood on day 30 after infection and they behaved normally and appeared healthy. One of the mice had 11% blood parasitemia on day 30, and one mouse in this group died on day 29. Of high medicinal importance, the efficacy of this ACT chemotherapy is much better than (almost double) the efficacy under the same conditions using as a positive control the popular trioxane drug artemether plus mefloquine hydrochloride (average survival time of only 16.5 days).
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影响因子：
2.7
作者：
Jung, M;Lee, S
通讯作者：
Lee, S
影响因子：
--
作者：
Lee, Seokjoon;Oh, Sangtae;Choi, Han-Kyu
通讯作者：
Choi, Han-Kyu
影响因子：
15.8
作者：
Delves M;Plouffe D;Scheurer C;Meister S;Wittlin S;Winzeler EA;Sinden RE;Leroy D
通讯作者：
Leroy D
影响因子：
2.7
作者：
Ban, Kung;Duffy, Sandra;Baell, Jonathan B.
通讯作者：
Baell, Jonathan B.
影响因子：
56.9
作者：
KLAYMAN, DL
通讯作者：
KLAYMAN, DL