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Characterization of the Alkylation Product of Heme by the Antimalarial Drug Artemisinin
Author(s) -
Robert Anne,
Cazelles Jérôme,
Meunier Bernard
Publication year - 2001
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/1521-3773(20010518)40:10<1954::aid-anie1954>3.0.co;2-9
Subject(s) - artemisinin , heme , alkylation , drug , chemistry , combinatorial chemistry , malaria , pharmacology , plasmodium falciparum , biology , biochemistry , immunology , enzyme , catalysis
The carbon‐centered radical 1 of the antimalarial drug artemisinin is generated after activation by reduced heme 2 (only scaffold shown), and is able to alkylate the heme macrocycle at the meso positions. Alkylation occurs preferentially at the α , β , or δ positions.