Halogenated analogs of the antimalarial bialamicol

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)]


Published in:
Synthesis, 5, 591-593
Year:
1996
Keywords:
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
0039-7881
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)
Laboratories:




 Record created 2006-03-03, last modified 2018-01-27


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