In a successful attempt to amplify the pharmacol. activity of the antimalarial bialamicol, substituents were introduced in the 2-position of the allyl side chains. 2-Fluoroallyl bromide, a versatile C3F building block, is described for the first time. While introduction of halogens did not alter the pharmacol. activity, addn. of HBr to the vinyl groups or substitution with Me induce a 500 and 100-fold increase of activity against Leishmania and Trypanosoma, resp. [on SciFinder (R)]
Titre
Halogenated analogs of the antimalarial bialamicol
Publié dans
Synthesis
Numéro
5
Pages
591-593
Date
1996
ISSN
0039-7881
Note
CAN 125:86251
25-7
Benzene, Its Derivatives, and Condensed Benzenoid Compounds
Institut de Chimie organique de l'Universite Batiment de Chimie (BCh),Lausanne-Dorigny,Switz.
Journal
written in English.
78-88-6 (2-Chloroallyl chloride); 92-88-6 (4,4'-Biphenyldiol); 106-95-6 (Allyl bromide); 513-31-5 (2-Bromoallyl bromide); 563-47-3 (2-Methylallyl chloride); 5675-31-0 Role: RCT (Reactant), RACT (Reactant or reagent) (prepn. of halogenated analogs of antimalarial bialamicol and activity against Leishmania and Trypanosoma); 3624-96-2DP (Bialamicol hydrochloride); 6942-01-4P; 35386-83-5P; 41481-62-3P; 149764-25-0P; 149764-26-1P; 178426-54-5P; 178426-55-6P; 178426-56-7P; 178426-57-8P; 178426-58-9P; 178426-59-0P; 178426-60-3P; 178426-64-7P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. of halogenated analogs of antimalarial bialamicol and activity against Leishmania and Trypanosoma); 3624-96-2P; 178426-61-4P; 178426-62-5P; 178426-63-6P; 178426-65-8P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of halogenated analogs of antimalarial bialamicol and activity against Leishmania and Trypanosoma)
Date de création de la notice
2006-03-03
