title: 1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: synthesis and antimalarial evaluation.
abstract: A series of 1H-1,2,3-triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates have been synthesized and evaluated for their antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum. The most potent of the test compound with an optimum combination of 3-hydroxy-indole ring and a n-butyl linker displayed an IC50 value of 69 nM.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
authors.forename: Raghu
authors.initials: R
authors.lastname: Raj
authors.affiliation: Department of Medicine, University of California, San Francisco, CA, USA.
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.affiliation: Department of Medicine, University of California, San Francisco, CA, USA.
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India. Electronic address: vipan_org@yahoo.com.
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004351:Drug Resistance; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007510:Isatin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D006834:Hydrazines; D007211:Indoles; D011804:Quinolines; D014230:Triazoles; D007510:Isatin; C030374:indole; D002738:Chloroquine
keywords: 1H-1,2,3-Triazole; 3-Hydroxy-indole-2-one; 7-Chloroquinoline; Antimalarial activity; Isatin