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 clinical randomized trial on dihydroartemisinin piperaquin was conducted with drug resistant malaria patients. The effectiveness to cure the disease through 56 days follow up the recurrent by PCR manifested on 97.4% in DTP group and 100% in A3M group. In second study the rate of recovery was equal in all groups - DTP group 97.4%; DP group 98.7%; A3M group 98.7%. Dihydroartemisenin piperaquin was well tolerated. In less than 3% of patients, there was side effects which can be related to smoking. The preparation is inexpensive, effective, safe with high efficacy to drug resistant malaria parasite.
Multidrug-Resistant ; artemisinins

The study was carried out on 100 healthy rats, weight of 12020g which were divided into 10 groups. Raw materials: BB103 pure powder and mefloquine. Results: In rats received BB103 with doses of 50 mg/kg and mefloquine 50 mg/kg in 5 days, there were no significant changes on process of conditioned reflex, speed of reflex establishment was stable, response time and extinguishing time of reflex were similar to those of the control group (p>0.05). In rats received BB103 with doses of 100 mg/kg and mefloquine 100 mg/kg in 5 days, there were significant changes on speed of reflex establishment and response time (p<0.01-0.05). There were differences on speed of reflex establishment, speed of stable reflex in rats received BB103 and mefloquine (p<0.01-0.05)
Artemisinins ; Rats ; Animal Experimentation

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 ;

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