Studying semi synthesis of some substances which contains lactam frame of artemisinin is 11-azaartemisinin, by let artemisinin interact with ammoniac or 3 amino including n-polyamine, n-butylamin and allylamin. The first step which was opening lacton circle to create amids occurred very fast within 30-45 minutes at room temperature. The second step which was closing circle occurred relatively low, usually 20-25 hours with the presence of strong acid catalyst. The higher temperature was, the lower the rates of 11-azaartemisinin derivatives were. The study was successful in transforming artemisinin into 11-azaartemisinin derivatives
Artemisinins ; Malaria

We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial activities than those shown by the derivatives having electron-donating groups. In particularly, m-chlorotriazolyl artemisinin (9d-12d) showed antimalarial activity equivalent to that of artemisinin and could be a strong drug candidate.
Artemisinins ; Cycloaddition Reaction ; Parasites

A high therapeutic efficacy was found in the experimental mouse model infected with P. berghei (both chloroquin sensitive and resistant strains). At a low dose, as twice as the human dose and calculated as mg/kg of body weight of mice, the combination produced a high effect, clearing parasite within 3 days. However a considerable rate of recrudescence (10%) was found within 28 following-up days. At a high dose as tenth as a human dose, the combination was found to have a high therapeutic effect of 100% cure rate on mice clearing parasite within 2 days and no recurrence occured within 28 following-up days in all the tests. Arterakin was found to be a highly effective antimalaria drug with cure rate of 100% and a fast parasite clearance time (1-2 days) in both P falciparum and P. vivax infected patients. The total dose of 8 tablets for 3 days for adults and relevant doses for children appeared to be appropriate
Malaria ; Therapeutics ; Artemisinins

The study was conducted to assess the effectiveness of the artesunate in 7-day treatment course on uncomplicated P.falciparum malaria from August to December 2003, in the Phuoc Hoa and Phuoc Thang communes, Bac Ai district, Ninh Thuan province. The clinical trials were implemented in conformity with the WHO Guidelines 2001. Artesunate with total dose of 16 mg/kg body weight was used for 7days in 159 patients with uncomplicated P. falciparum malaria. The oral treatment of patients was supervised strictly; the clinical assessment and parasite density were followed up during 28 days after treatment. The number of patients completing 28-day follow-up was 131 cases. The trial results showed that the success rate of treatment was 122/131 (accounting for 93.1%) cases, the mean fever clearance time (mean +/- SD) was 1.2:+/- 0.4 days, the mean parasite clearance time was 1.8+/- 0.7 days and the rate of late treatment failure was 9/131 cases (6.9%)
Malaria ; Malaria, ; Falciparum ; Artemisinins

Therapeutic efficacy of dihydroartemisinin (DHA) - piperaquin in treatment of P falciparum and P. vivax was investigated in the National Institute of Malariology, Parasitology and Entomology (NIMPE), Hospital of Tropical Diseases in Ho Chi Minh city. Hospital inpatients and patients in primary health care facilities were enrolled in the study. Four small scale clinical studies were conducted and followed by large scale treatment studies in the Hospital of Tropical Diseases and primary health care services in the provinces of Binh Phuoc, Dak Lak, Quang Tri during the period 2001 - 2004. A total number of 3,978 malaria patients (989 P. vivax and 2,999 P falciparum were sampled
Malaria ; Therapeutics ; Artemisinins

The BB134's sub-chronic toxicity in rabbits was investigated at NIMPE's laboratory. BB134 was orally administered at the dose of 9mg/kg of body weight per day for 28 consecutive days. The influence of BB134 on rabbit's laboratory indices and cardiovascular system were observed during and after the BB134 administration. The BB134 had not change the normal indices of development as well as the biochemical and some hematological indices of the experimental rabbits. During the study time the rabbits acted and ate normally. The body weight was increased significantly. SGOT, SGPT, bilirubin and creatinine as well as leukocytes, leukocyte formula and hemoglobin had no change. However erythrocytes decreased significantly by day 14. BB134 was also found not to affect significantly on rabbits' cardiovascular system (rabbits' heart rhythms and cardiovascular waves such as P, QP, QRS, T and QT of the control and treated groups were not changed significantly
Malaria ; Animal Experimentation ; Artemisinins

Quality of the locally produced artesunate 50mg tablets provided by the National Malaria Control program to five provinces of Cao Bang, Bac Kan, Ha Tinh and Ninh Thuan was monitored in a survey from June 2001 to December 2004 that was conformed with the expiry date of the drug. The drug had also been previously found to meet the quality criteria of manufacturer and pharmacopoeia. Analysis of samples collected from five provinces showed a remaining stable quality of mass equability, disintegration, hardness and solubility as permitted limits. The artesunate concentration was found to be 90-100% and 95-105% according to pharmaceutical classes and manufacturer criteria, respectively
Malaria ; Pharmaceutical Preparations ; Artemisinins

The synthesis of 10 beta-allyldeoxoartemisinin with excellent results through the intermediate dihydroartemisinin 10 alpha-benzoate using zinc chloride as catalyst was performed. This compound was then oxidized using osmium tetra oxide and oxone in dimethyl formamide to give 10 beta-(2'-carboxymethyl) deoxoartemisinin with high yield. Many important different derivatives of artemisinin can be synthesized from this important compound
Artemisinins ; Pharmaceutical Preparations

The sub-chronic toxicity of an antimalaria combination between piperaquine phosphate (PQP) and dihydroartemisinin (DHA) at the doses of 64 and 100 mg of (PQP+DHA)/kg of body weight/day for 28 consecutive days in rabbits was investigated in this study. Results: rabbits acted and ate normally. At the doses of 64 mg of (PQP+DHA)/kg/day x 28 consecutive days, the body weights of rabbits increased statistical significantly at day N28 compared to days before using the combination (p<0.05). At the doses of (PQP+DHA) 100 mg/kg/day x 28 consecutive days, the weights of rabbits increased statistically at day 14 and 28. At dose of 64 mg PQP+DHA/kg/day x 28 day, biochemical indicators (SGOT, SGPT, creatinin, protein and bilirubin) and hematological indicators (erythrocytes, leukocytes, leukocyte formula and hemoglobin) did not change significantly (p>0.05) after 28 days. At dose of 100 mg PQP+DHA/kg/day x 28 days, biochemical indicators (SGOT, SGPT, creatinin, protein and bilirubin) and hematological indicators (hemoglobin, erythrocytes, leukocytes, neutrophils and lymphocytes) did not change significantly (p>0.05) after 28 days but protein and monocytes increased significantly (p<0.05) on day 28
Malaria ; Therapeutics ; Artemisinins

65 patients with uncomplicated Pl.falciparum malaria were monitored during 28 days after 5 -day -course use of artemisinine (year 1998) and 69 patients after 7 day course (year 2001). The mean fever cut time lengthened for 1,5 days in 1998 and 1,8 days in 2001.The mean parasite cut time had lengthened for 1,8 days in1998 and 2,3 days in 2001. The rate of reappearance of parasite accounted for 36,9% within 28 days follow up with 5 -day -course procedure and 7,3 % with 7 days procedure. The rate of repeated infestion was remarkable: 10/21 patients (year1998) and 3/5 (year 2001) had got recurrence. No change of EC50 was reported between the years 1998 and 2001, but an increase by 2 and 4 folds of EC90 and EC99 was reported.EC50,90 and 99% of chloroquine, mefloquine and quinine in the year 2001 decreased by 2 folds vs 1998
malaria ; malaria, falciparum ; Artemisinins ;