Synthesis of limonene β-amino alcohol derivatives in support of new antileishmanial therapies

TY - JOUR

T1 - Synthesis of limonene β-amino alcohol derivatives in support of new antileishmanial therapies

AU - Ferrarini, Stela R

AU - Graebin, Cedric S

AU - Limberger, Jones

AU - Canto, Rômulo FS

AU - Dias, Daiane O

AU - da Rosa, Ricardo G

AU - De Fátima Madeira, Maria

AU - Eifler-Lima, Vera L

PY - 2008/12

Y1 - 2008/12

N2 - A series of seven limonene β-amino alcohol derivatives has been regioselectively synthesised in moderate to good yields. Two of these compounds were found to be significantly effective against in vitro cultures of the Leishmania (Viannia) braziliensis promastigote form in the micromolar range. The activities found for 3b and 3f were about 100-fold more potent than the standard drug, Pentamidine, in the same test, while limonene did not display any activity. This is the first report of antileishmanial activity by limonene β-amino alcohol derivatives.

AB - A series of seven limonene β-amino alcohol derivatives has been regioselectively synthesised in moderate to good yields. Two of these compounds were found to be significantly effective against in vitro cultures of the Leishmania (Viannia) braziliensis promastigote form in the micromolar range. The activities found for 3b and 3f were about 100-fold more potent than the standard drug, Pentamidine, in the same test, while limonene did not display any activity. This is the first report of antileishmanial activity by limonene β-amino alcohol derivatives.

KW - Leishmania braziliensis

KW - Leishmaniasis

KW - Limonene

KW - Neglected diseases

KW - Synthesis

KW - β-amino alcohol

UR - https://www.scopus.com/pages/publications/58049164442

U2 - 10.1590/S0074-02762008000800005

DO - 10.1590/S0074-02762008000800005

M3 - Article

C2 - 19148415

AN - SCOPUS:58049164442

SN - 0074-0276

VL - 103

SP - 773

EP - 777

JO - Memorias do Instituto Oswaldo Cruz

JF - Memorias do Instituto Oswaldo Cruz

IS - 8

ER -