title: β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation.
abstract: A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC50 values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity.
authors: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors: Nisha
authors: Department of Medicine, University of California, San Francisco, CA, USA.
authors: Jiri
authors: J
authors: Gut
authors: Department of Medicine, University of California, San Francisco, CA, USA.
authors: Philip J
authors: PJ
authors: Rosenthal
authors: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: vipan_org@yahoo.com.
authors: Vipan
authors: V
authors: Kumar
mesh_terms: D000605:Amino Alcohols / Q000737:chemistry / Q000494:pharmacology*; D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D045325:HCT116 Cells; D006801:Humans; D007510:Isatin / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000605:Amino Alcohols; D000634:Aminoquinolines; D000962:Antimalarials; D007510:Isatin; C001920:4-aminoquinoline
keywords: 4-Aminoquinoline-isatin conjugates; Antimalarial activity; Cytotoxicity; β-amino alcohol