title: Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors.
abstract: Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14,17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as potential antimalarial drugs.
authors.affiliation: Pharmacy Department, Faculty of Tech. and Engg., The M S University of Baroda, Vadodara 390 001,Gujarat, India.
authors.forename: U R
authors.initials: UR
authors.lastname: Mane
authors.forename: H
authors.initials: H
authors.lastname: Li
authors.forename: J
authors.initials: J
authors.lastname: Huang
authors.forename: R C
authors.initials: RC
authors.lastname: Gupta
authors.forename: S S
authors.initials: SS
authors.lastname: Nadkarni
authors.forename: R
authors.initials: R
authors.lastname: Giridhar
authors.forename: P P
authors.initials: PP
authors.lastname: Naik
authors.forename: M R
authors.initials: MR
authors.lastname: Yadav
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003546:Cysteine Endopeptidases / Q000378:metabolism*; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology* / Q000254:growth & development; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D015853:Cysteine Proteinase Inhibitors; D011744:Pyrimidinones; D003546:Cysteine Endopeptidases; C416224:falcipain 2