ライフサイエンスコーパス: trioxane

1 grees C of 2,4,6-tri(propan-2-ylidene)-1,3,5-trioxane.

2 r than that for a corresponding six-membered trioxane.

3 Almost exclusive formation of the trioxane 12alpha-stereoisomers simplifies product purifi

4 e oral dose of only 6 mg/kg of the monomeric trioxane 12c combined with 18 mg/kg of mefloquine hydroc

5 cyclohexane (1), r-2,c-4,c-6-trifluoro-1,3,5-trioxane (2), and r-2,c-4,c-6-trifluoro-1,3,5-trithiane

6 1,3,5-Trioxane-2,4,6-trione (cyclic trimer of CO2) is the prod

7 A new series of bile acid-based trioxanes 23a-d, 24a-d, 25a-d, 26a, 26b, and 26d have be

8 The more polar diastereomer of the trioxanes 26a, 26b, and 26d, were the most active compou

9 nistration, these new synthetic antimalarial trioxanes 3 and 5 are 14-20 times more soluble in water

10 one oral dose of only 6.8 mg/kg of monomeric trioxane 4b combined with 20 mg/kg of mefloquine hydroch

11 acy of this ACT chemotherapy using monomeric trioxane 4b plus mefloquine hydrochloride is considerabl

12 a series of structurally simple 3-aryl-1,2,4-trioxanes 5 was designed and was prepared in three to fi

13 dispiro-1,2,4-trioxolane 4 and dispiro-1,2,4-trioxanes 5-7 with ferrous bromide and 4-oxo-TEMPO.

14 Unexpectedly, two thiazole trioxanes (5 and 6) were parasiticidal; both inhibited p

15 Novel C4-(hydroxyalkyl)trioxanes 5d and 5e were designed and synthesized based

16 potent, with crystalline fluorobenzyl ether trioxane 5k especially potent even when administered to

17 cally complementary fashion, 3-(fluoroalkyl)-trioxanes 6 were prepared via attachment of electrophili

18 l evaluation of this water-soluble synthetic trioxane 8a in rodents shows it to have at least as good

19 pharmacologically critical peroxide unit in trioxane 8a.

20 -10 non-acetal dimers were prepared from key trioxane alcohol 10beta-(2-hydroxyethyl)deoxoartemisinin

21 ivatives 6, 7, and 21 of C4 beta-substituted trioxane alcohols 4a, 5d, and 5e were prepared, each in

22 nd ADME profiles of the 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.

23 The currently accepted mechanism of trioxane antimalarial action involves generation of free

24 chemical syntheses of four new antimalarial trioxanes are presented, starting with inexpensive and c

25 city) as that of water-soluble semisynthetic trioxane artelinic acid (5).

26 63% overall yield, naturally occurring 1,2,4-trioxane artemisinin (1) was converted into C-10-carba t

27 nd in 70% overall yield, naturally occurring trioxane artemisinin (1) was converted on a gram scale i

28 e C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using s

29 ng 140 to 50% of the efficacy of the natural trioxane artemisinin (1).

30 sulfones has been prepared from the natural trioxane artemisinin in five or six chemical steps.

31 gically and prepared easily from the natural trioxane artemisinin in only four or five chemical steps

32 rresponding 1,2,4-trioxolane 1 and the 1,2,4-trioxane artemisinin undergo primarily one-electron iron

33 xteen new anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for ant

34 n four or five chemical steps from the 1,2,4-trioxane artemisinin, a new series of 23 trioxane dimers

35 nd in 21-67% overall yields from the natural trioxane artemisinin, a series of 21 new trioxane C-10 t

36 steps and 48% overall yield from the natural trioxane artemisinin, the thermally and hydrolytically s

37 bed here represent effective anti-Toxoplasma trioxanes as well as molecular probes for elucidating th

38 ral trioxane artemisinin, a series of 21 new trioxane C-10 thioacetals was prepared.

39 This simplified acetal trioxane carboxylic acid 8a is thermally stable, and it

40 rtemisinin (1) was converted into C-10-carba trioxane conjugated diene dimer 4.

41 ve prepared 23 new dehydroartemisinin (DART) trioxane derivatives (11 thiazoles, 2 oxadiazoles, and 1

42 as converted on a gram scale into C-10-carba trioxane dimer 3.

43 this trioxane dimer 4c as well as its parent trioxane dimer 4b also completely cured malaria-infected

44 h 13 mg/kg of mefloquine hydrochloride, this trioxane dimer 4c as well as its parent trioxane dimer 4

45 echanisms of action of three C-10 non-acetal trioxane dimers (TDs) were examined in human (LNCaP) and

46 ps from naturally occurring artemisinin (1), trioxane dimers 6 and 7 were prepared on a multigram sca

47 Ten new trioxane dimers at only a single oral dose of 30 mg/kg p

48 Four of these trioxane dimers cure malaria-infected mice after only a

49 Eleven of these new trioxane dimers cure malaria-infected mice via oral dosi

50 rcinoma of mouse prostate model, some of the trioxane dimers had potent anticancer activity.

51 2,4-trioxane artemisinin, a new series of 23 trioxane dimers has been prepared.

52 the curative activity of a new generation of trioxane dimers, designed logically and prepared easily

53 ions using as a positive control the popular trioxane drug artemether plus mefloquine hydrochloride (

54 under the same conditions using the popular trioxane drug artemether plus mefloquine hydrochloride.

55 ing semisynthetic, herb-derived antimalarial trioxane drug candidate.

56 The clinically used trioxane drug sodium artesunate prolonged mouse average

57 icroM of drug for 24 h, whereas the standard trioxane drugs artemisinin and artemether were not paras

58 nin, the thermally and hydrolytically stable trioxane fluoroanilide 4b has been prepared.

59 ADME profiles in the rank order trioxolane > trioxane > tetraoxane.

60 Single electron reduction of the 1,2,4-trioxane heterocycle of artemisinin (1) forms primary an

61 armacophoric peroxide bond in a unique 1,2,4-trioxane heterocycle.

62 For the OZ277 series, the trioxane isostere had the best ADME profile, but its ove

63 In only three chemical operations, natural trioxane lactone artemisinin (1) was converted into a se

64 mistry at C3 and C6 (C21 in Figure 5) of the trioxane moiety.

65 he two diastereomers isolated of each of the trioxanes, more polar one was significantly more active

66 ion of 2,4,6-tris(2-chloropropan)-2-yl-1,3,5-trioxane; ozonolysis at -80 degrees C of 2,4,6-tri(propa

67 ssed poor anticancer activity apart from the trioxane phosphate ester dimers 14a and 14b, which expre

68 The resulting 1,2,4-trioxane products were derivatized and show potent cance

69 All these three trioxanes provided 100% protection at 24 mg/kgx4 days.

70 n vivo antimalarial evaluations of these new trioxanes showed 12 beta-methoxy-3-aryltrioxanes 5g, 5j,

71 The antimalarial activity of these trioxanes showed a strong dependence on the side-chain l

72 lecular mechanism of action of similar 1,2,4-trioxanes structurally related to the antimalarial natur

73 A new series of 6 dimeric trioxane sulfones has been prepared from the natural tri

74 %) by reacting sulfamide with H(14)CHO and s-trioxane then completion of the sequential cyclization w

75 This trioxane-trione is detected in solution at temperatures

76 observation emphasizes the importance of two trioxane units for high antiproliferative activity, and

77 ly diastereoselective aldol reactions with s-trioxane were also achieved with N-acyl thiazolidinethio