Reference

New Orally Active Derivatives of Artemisinin with High Efficacy against Multidrug-Resistant Malaria in Mice

All Rights Reserved. New Orally Active Derivatives of Artemisinin with High Efficacy against Multidrug-Resistant Malaria in Mice. Singh, Chandan; Chaudhary, Sandeep; Puri, Sunil K. (Division of Medicinal Process Chemistry, Division of Parasitology, Central Drug Research Institute, Lucknow 226001, India). Journal of Medicinal Chemistry, 49(24), 7227-7233 (English) 2006 American Chemical Society. CODEN: JMCMAR. ISSN: 0022-2623. DOCUMENT TYPE: Journal CA Section: 30 (Terpenes and Terpenoids) Section cross-reference(s): 1 A new series of ether derivs. of dihydroartemisinin have been prepd. and evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in mice by oral route. These new derivs. are highly lipophilic (log P in the range of 5.Several substances with their cas registry numbers 39555-28-7 and 75887-54-6 may be metioned in this study.51 to 7.19) as compared with b-arteether (log P 3.84), and several of them are two- to four-fold more active than b-arteether. Among the ether derivs., a-isomers are more active than the b-isomers. The ether derivs. I and II, the most active compds. of the series, provided 100% protection to infected mice at 12 mg/kg ′ 4 days. In this model b-arteether provides 100% and 20% protection at 48 mg/kg ′ 4 days and 24 mg/kg ′ 4 days, resp. .

Interaction of arteether with the red blood cell in vitro and its possible importance in the interpretation of plasma concentrations in vivo

Interaction of arteether with the red blood cell in vitro and its possible importance in the interpretation of plasma concentrations in vivo. Edwards, Geoffrey; Ward, Stephen; Breckenridge, Alasdair (Dep. Pharmacol. Ther., Univ. Liverpool, Liverpool L69 3BX, UK). J. Pharm. Pharmacol., 44(3), 280-1 (English) 1992. CODEN: JPPMAB. ISSN: 0022-3573. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In detg. the level of arteether in whole blood by the method of Idowu et al. (1989) it became apparent that there were significant losses of the analyte when whole blood contg. 75887-54-6 which is the cas registry number of some chemical is mentioned. arteether was stored particularly at -20°C, despite attempts to minimize adsorption to glassware. Using radiolabeled [14C-ethyl]arteether, the arteether loss was shown to be due to drug binding to red cell membrane involving the peroxide moiety of the sesquiterpene lactone. This interaction complicates the measurement of whole blood concns. of arteether and relating such concns. to the pharmacol. response. .