Research Publications (Applied Sciences)

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Urea/oxalamide tethered b-lactam-7-chloroquinoline conjugates: Synthesis and in vitro antimalarial evaluation
(Elsevier, 2013-11-09) Singh, Pardeep; Raj, Raghu; Singh, Parvesh; Gut, Jiri; Rosenthal, Philip J.; Kumar, Vipan
The manuscript pertains to the synthesis of urea/oxalamide tethered b-lactam-7-chloroquinoline con-jugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity proﬁles on the N-1 substituent of the b-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.
Azide-alkyne cycloaddition en route to 1H-1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras : synthesis and antimalarial evaluation
(Elsevier, 2013-04) Raj, Raghu; Singh, Pardeep; Singh, Parvesh; Gut, Jiri; Rosenthal, Philip J.; Kumar, Vipan
We describe the synthesis and antimalarial activities of 1H-1,2,3-triazole tethered 7-chloroquinoline-isatin hybrids. Activity against cultured parasites was dependent on the C-5 substituent of the isatin ring as well as the alkyl chain length between the isatin and 7-chloroquinoline moieties. Compound 8h, with an optimum alkyl chain length (n = 3) and a chloro substituent at the C-5 position of the isatin ring, displayed the best activity among the test compounds, with IC50 value of 1.21 μM against cultured W2-strain Plasmodium falciparum.