Modifications of the alpha,beta-double bond in chalcones only marginally affect the antiprotozoal activities

TY - JOUR

T1 - Modifications of the alpha,beta-double bond in chalcones only marginally affect the antiprotozoal activities

AU - Nielsen, S F

AU - Kharazmi, A

AU - Christensen, S B

N1 - Keywords: Animals; Antimalarials; Chalcone; Erythrocytes; Leishmania major; Plasmodium falciparum; Structure-Activity Relationship; Trypanocidal Agents

PY - 1998

Y1 - 1998

N2 - Methods for selective alkylation of chalcones in the alpha- or beta-position and for selective reduction of the alpha,beta-double bond have been developed. The antiparasitic potencies of the alpha,beta-double bond modified chalcones only differ marginally from the potencies of the parent chalcones indicating that the propenone residue only functions as a spacer between the two benzene rings, which are the true pharmacophore.

AB - Methods for selective alkylation of chalcones in the alpha- or beta-position and for selective reduction of the alpha,beta-double bond have been developed. The antiparasitic potencies of the alpha,beta-double bond modified chalcones only differ marginally from the potencies of the parent chalcones indicating that the propenone residue only functions as a spacer between the two benzene rings, which are the true pharmacophore.

M3 - Journal article

C2 - 9730229

SN - 0968-0896

VL - 6

SP - 937

EP - 945

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 7

ER -