74509-63-0Relevant academic research and scientific papers
Antimalarials. 16. Synthesis of 2-substituted analogues of 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3- (trifluoromethyl)phenoxy]quinoline as candidate antimalarials
LaMontagne,Blumbergs,Smith
, p. 1728 - 1732 (2007/10/02)
A series of 2-substituted analogues of the exceptional drug 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3- (trifluoromethyl)phenoxy]quinoline (I) were prepared and evaluated for both suppressive and prophylactic antimalarial activity. The preparation of analogues of compound I was of interest due to the high level of both blood and tissue schizonticidal activity demonstrated by this compound. One analogue, 8a, was found to be both more active and less toxic than the parent compound I. In addition, three analogues of example 8a were prepared. Although two of the three analogues showed significant antimalarial activity, both were inferior to compound 8a.
Analogues of 8-amino>-6-methoxy-4-methylquinoline as Candidate Antileishmanial Agents
LaMontagne, Maurice P.,Dagli, Dinesh,Khan, M. Sami,Blumbergs, Peter
, p. 981 - 985 (2007/10/02)
8-amino>-6-methoxy-4-methylquinoline (I) has been shown to be highly effective against Leishmania donovani in hamsters, being approximately 475 times as active as the standard meglumine antimoniate.Several nuclear and side-chain analogues of I have been prepared in an attempt to further enhance the antileishmanial activity of this class of compounds.The compounds were tested against L. donovani in the golden hamster.Although several analogues had meglumine antimoniate indexes in excess of 300, none was superior to the model compound.
