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Miscellaneous

Preparation of chemically robust new artemisinin derivatives

Pages 1763-1769 | Published online: 02 Mar 2005

Bibliography

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  • ••A marvellous, highly analytical andperceptive overview, which gives the problems of current drugs and the potential for development of new drugs for malaria, based on mechanism of action.
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  • ••This is a comprehensive and relativelywell-balanced review, which places contributions from the various research groups in relation to synthesis, biological activity and mechanism of action in proper perspective.
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  • ••This paper provides a comprehensivequantitative structure-activity relationship analysis of most artemisinin derivatives, many of which have been prepared by the Avery group by carefully planned, well-executed total synthesis.
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  • •This paper, together with reference [14] and an earlier patent, Au P6989 (September 1989), describe the first examples of this conversion, which has been used elsewhere for making artemisinin derivatives ([16]).
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  • •The preparation of the titled derivative uses the oxygenation method described in [13–15].
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  • ••This very nice publication reveals apotential problem with protracted dose regimens involving artemisinin derivatives that provide DHA upon metabolism.
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  • ••An excellent paper, which clearly presentsvery good synthetic transformations without the use of the overwrought hyperbole characterising publications from some other groups working in the artemisinin synthesis area.
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  • •Acquisition of pharmacokinetic parameters for the titled compound would be of some interest. Like the other trifluoromethylated artemisinin derivatives from this group, the compound is anticipated to have a longer half-life than current derivatives.
  • GRELLEPOIS F, CHORKI F, OUREVITCH M, CROUSSE B, BONNET-DELPON D, BEGUE JP: Allyfic bromination of anhydrodihydroartemisinin and of its 10-trifluoromethyl analogue: a new access to 16-substituted artemisinin derivatives. Tetrahedron Letters (2002) 43:7837–7840.
  • •The compounds are predicted to be relatively very stable as compared to current artemisinin derivatives.
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