title: New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents.
abstract: A novel series of dihydropyrimidines (DHPMs) 4a-j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC50 values ranging from 0.014-5.87 μg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ).
authors.affiliation: Chemistry Department, Faculty of Science, Jazan University, Jazan 2097, Saudi Arabia. iradini4@gmail.com.
authors.forename: Ibrahim Ali M
authors.initials: IA
authors.lastname: Radini
authors.affiliation: Biology Department, Faculty of Science, Jazan University, Jazan 2097, Saudi Arabia. telsheikh1964@yahoo.com.|Department of Zoology, Faculty of Science, Al-Azhar University, Cairo 11675, Egypt. telsheikh1964@yahoo.com.
authors.forename: Tarek M Y
authors.initials: TM
authors.lastname: Elsheikh
authors.affiliation: Chemistry Department, Faculty of Science, Jazan University, Jazan 2097, Saudi Arabia. dremade1966@yahoo.co.uk.|Chemical Industries Division, National Research Centre, Dokki 12622, Giza, Egypt. dremade1966@yahoo.co.uk.
authors.forename: Emad M
authors.initials: EM
authors.lastname: El-Telbani
authors.affiliation: Chemistry Department, Faculty of Science, Jazan University, Jazan 2097, Saudi Arabia. rizkkhidre@yahoo.com.|Chemical Industries Division, National Research Centre, Dokki 12622, Giza, Egypt. rizkkhidre@yahoo.com.
authors.forename: Rizk E
authors.initials: RE
authors.lastname: Khidre
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D020128:Inhibitory Concentration 50; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011804:Quinolines
keywords: Biginelli reaction; Plasmodium falciparum; antimalarial activities; dihydropyrimidines; quinoline-4-carbaldehyde