title: Emergence of pyrido quinoxalines as new family of antimalarial agents.
abstract: A series of novel N-alkyl dihydro pyrido quinoxaline derivatives were synthesized using Gould-Jacobs reaction and evaluated their antimalarial activity in vitro against chloroquine sensitive (3D7) and drug resistant (Dd2) strains of Plasmodium falciparum. Among the compounds tested, 10 compounds were more potent than their structural standard analog ciprofloxacin, including 2 derivatives 5e and 5h, which showed 3.3-7.4 times more potency than ciprofloxacin against both the parasite strains. The results are encouraging and a lead molecule may emerge which is useful alone or in combination therapy.
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
authors.forename: A
authors.initials: A
authors.lastname: Chandra Shekhar
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. Electronic address: shanthanpp1954@gmail.com.
authors.forename: P
authors.initials: P
authors.lastname: Shanthan Rao
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
authors.forename: B
authors.initials: B
authors.lastname: Narsaiah
authors.affiliation: CSIR-Centre for Cellular and Molecular Biology, Hyderabad 500 007, India.
authors.forename: Aparna Devi
authors.initials: AD
authors.lastname: Allanki
authors.affiliation: CSIR-Centre for Cellular and Molecular Biology, Hyderabad 500 007, India.
authors.forename: Puran Singh
authors.initials: PS
authors.lastname: Sijwali
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004912:Erythrocytes / Q000187:drug effects / Q000382:microbiology; D006801:Humans; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011719:Pyrazines; D011810:Quinoxalines
keywords: Antimalarial activity; Gould–Jacobs reaction; Plasmodium falciparum; Pyrido quinoxaline; Quinolones