title: 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies.
abstract: A new series of 4-aminoquinoline derivatives have been synthesized and found to be active against both susceptible and resistant strains of Plasmodium falciparum in vitro. Compound 1-[3-(7-chloro-quinolin-4-ylamino)-propyl]-3-cyclopropyl-thiourea (7) exhibited superior in vitro activity against resistant strains of P. falciparum as compared to chloroquine (CQ). All the compounds showed resistance factor between 0.59 and 4.31 as against 5.05 for CQ. Spectroscopic studies suggested that this class of compounds act on heme polymerization target.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, MG Road, Lucknow 226 001, India.
authors.forename: V R
authors.initials: VR
authors.lastname: Solomon
authors.forename: W
authors.initials: W
authors.lastname: Haq
authors.forename: M
authors.initials: M
authors.lastname: Smilkstein
authors.forename: Kumkum
authors.initials: K
authors.lastname: Srivastava
authors.forename: Sunil K
authors.initials: SK
authors.lastname: Puri
authors.forename: S B
authors.initials: SB
authors.lastname: Katti
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006418:Heme / Q000037:antagonists & inhibitors* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects; D011108:Polymers / Q000737:chemistry*; D016339:Spectrometry, Mass, Fast Atom Bombardment
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D011108:Polymers; D006418:Heme; C001920:4-aminoquinoline