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

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 ;

Investigating the influence of trifluoromethylhydroartemisinin (BB.101) on chromosome mutations of mice. Mices were divided into 4 batches (B1, B2, B3 were dosed with BB.101 50mg/kg/day x 5 days, once, twice and thrice, respectively; each treatment course was repeated with 7 days intervals. B4 (control) were tested with arabic gum emulsion 1%). The results showed that: BB.101 were found not to increase frequency of confused chromosome in bone marrow cells of mices. Cells with confused structures and trouble clusters as crushed and smudged chromosomes were not found. BB.101 with the same dose was found not to increase frequency of confused chromosome in testicle cells of mices
Chromosomes ; Mice ; artemisinins

At the dose of 4 and 8 mg/kg/day for 30 consecutive days, the monkeys appeared to have normal living actions taking meals and drink. Their body weights did not change significantly. At the dose of 4mg/kg/day for 30 consecutive days, changes of SGOT and creatinine indices were not significant but erythrocyte, reticulocyte, leucocyte and SGPT indices changed significantly. These indices became normal 15 days after interruption of the drug administration. At the dose of 8 mg/kg/day for consecutive 30 days, the changes of SGOT index was not significant during the administration. Haemoglobin, erythrocyte, reticulocyte, leucocyte, SGPT and creatinine indices were significantly changed during the 30 days administration. Haemoglobin, erythrocyte, reticulocyte, SGPT and creatinine indices changed significantly but erythrocyte and leucocyte indices became normal 15 days after the drug administration
Toxicity ; animals ; Haplorhini ; Artemisinins

The study examined some factors (solvent, catalysis, temperature) affecting to fluoroalkyl ether subsynthesis effects of dihydroartemisinin. TF-DHA and PF-DHA, two fluoroalkylether derivatives of dihydroartermisinin was prepared by treatment of dihydroartermisin with appropriate fluoroalcohol in the presence of boron trifluoride etherate. The dicloromethan solvent is most efficient option for TF-DHA's preparation
Artemisinins ; Therapeutics ; Solvents

Artesunat at doses of 50 mg/kg the first day and 25 mg/kg per day for four following days had no effect to the birth progress of P, F1 and F2. Concretely: No coffuse birth: ratio of conjugation, conception, early died feotus and late died feotus among P, F1 and F2 were similar, and were not higher than control group. No innate defects in born mice from P, F1 and F2. Quantity and weight of mice were in normal, and were not different with the control group
Artemisinins ; Pharmaceutical Preparations ; Therapeutics

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