title: 7-chloroquinoline-isatin conjugates: antimalarial, antitubercular, and cytotoxic evaluation.
abstract: A series of twenty piperazine-tethered 7-chloroquinoline-isatin hybrids have been synthesized via either direct nucleophilic substitution or Cu(Ι)Cl-mediated Mannich reaction. These new conjugates were evaluated for their antimalarial and antitubercular efficacy against a chloroquine-resistant strain of Plasmodium falciparum and Mycobacterium tuberculosis, respectively, while the cytotoxic profiles were evaluated against 3T6 cell line, a permanent mouse embryonic fibroblast cell line. The most potent of the test compound with IC50 of 0.22 μm against W2 strain of P. falciparum and 31.62 μm against the embryonic fibroblast cell line (cytotoxicity) displayed a high selective index of 143.73.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar, Punjab, 143005, India.
authors.forename: Raghu
authors.initials: R
authors.lastname: Raj
authors.forename: Christophe
authors.initials: C
authors.lastname: Biot
authors.forename: Séverine
authors.initials: S
authors.lastname: Carrère-Kremer
authors.forename: Laurent
authors.initials: L
authors.lastname: Kremer
authors.forename: Yann
authors.initials: Y
authors.lastname: Guérardel
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.forename: Delphine
authors.initials: D
authors.lastname: Forge
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002738:Chloroquine / Q000737:chemistry*; D004351:Drug Resistance; D007510:Isatin / Q000737:chemistry*; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D000995:Antitubercular Agents; D007510:Isatin; D002738:Chloroquine
keywords: 7-chloroquinoline-isatin scaffolds; antimalarial activity; antitubercular activity; cytotoxicity; structure activity relationship