Urea/oxalamide tethered beta-lactam-7-chloroquinoline conjugates: Synthesis and in vitro antimalarial evaluation

作者：Singh Pardeep; Raj Raghu; Singh Parvesh; Gut Jiri; Rosenthal Philip J; Kumar Vipan^*

来源：European Journal of Medicinal Chemistry, 2014, 71: 128-134.

DOI：10.1016/j.ejmech.2013.10.079

• beta-Lactam-7-chloroquinoline conjugates
• Urea/oxalamide linker
• Antimalarial evaluation
• Structure-activity relationship

The manuscript pertains to the synthesis of urea/oxalamide tethered beta-lactam-7-chloroquinoline conjugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity profiles on the N-1 substituent of the beta-lactam ring, the nature of the linker as well as the length of the alkyl chain. The most potent of the tested compounds showed an IC50 of 34.97 nM against chloroquine resistant W2 strain of Plasmodium falciparum.

• 出版日期2014-1