Sf. Nielsen et al., MODIFICATIONS OF THE ALPHA,BETA-DOUBLE BOND IN CHALCONES ONLY MARGINALLY AFFECT THE ANTIPROTOZOAL ACTIVITIES, Bioorganic & medicinal chemistry, 6(7), 1998, pp. 937-945
Methods for selective alkylation of chalcones in the alpha- or beta-po
sition and for selective reduction of the alpha,beta-double bond have
been developed. The antiparasitic potencies of the alpha,beta-double b
ond modified chalcones only differ marginally from the potencies of th
e parent chalcones indicating that the propenone residue only function
s as a spacer between the two benzene rings, which are the true pharma
cophore. (C) 1998 Elsevier Science Ltd. All rights reserved.