title: Synthesis and antimalarial activity of N-benzylated (N-arylcarbamoyl)alkylphosphonic acid derivatives.
abstract: A series of novel and readily accessible N-benzylated (N-arylcarbamoyl)alkylphosphonate esters and related compounds have been prepared as potential antimalarial agents. Bioassays reveal that some of these compounds exhibit promising activity against Plasmodium falciparum, and exhibit no significant growth inhibition of HeLa cells.
authors: Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
authors: Christiana M
authors: CM
authors: Adeyemi
authors: Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
authors: Faridoon
authors: Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
authors: Michelle
authors: M
authors: Isaacs
authors: Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
authors: Dumisani
authors: D
authors: Mnkandhla
authors: Department of Biochemistry and Microbiolgy, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
authors: Heinrich C
authors: HC
authors: Hoppe
authors: Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
authors: Rui W M
authors: RW
authors: Krause
authors: Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. Electronic address: P.Kaye@ru.ac.za.
authors: Perry T
authors: PT
authors: Kaye
mesh_terms: D019747:Aldose-Ketose Isomerases / Q000037:antagonists & inhibitors; D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D000962:Antimalarials / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D005578:Fosfomycin / Q000031:analogs & derivatives / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D063065:Organophosphonates / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000962:Antimalarials; D063065:Organophosphonates; D005578:Fosfomycin; C024639:3-(N-acetyl-N-hydroxy)aminopropylphosphonic acid; C114231:1-deoxy-D-xylulose 5-phosphate reductoisomerase; D019747:Aldose-Ketose Isomerases
keywords: Anti-malarial; Aryl and heteroaryl derivatives; N-Benzylated phosphonate esters; PfDXR