title: 2-[(18)F]-fluoroisonicotinic acid hydrazide: biological evaluation in an acute infection model.
abstract: We have synthesized 2-[(18)F]-fluoroisonicotinic acid hydrazide by nucleophilic displacement reaction on ethyl-2- (trimethylammonium)-isonicotinate precursor in acetonitrile. Kryptofix 222 was used as the phase transfer catalyst. The intermediate fluorinated ethyl ester reacted with hydrazine hydrate to produce the hydrazide. Excellent radiochemical yield was attained with total synthesis time of approximately 60 min. Biological evaluation was performed in bacterial cells and biodistribution in normal as well as E. coli infected CBA/J mice. It was found that the S. pneumoniae cells retained the radiotracer in an in vitro assay. The tracer showed positive localization at the infection/inflammation site in E. coli infected mice.
authors.affiliation: Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, MBC-03, P.O. Box 3354, Riyadh 11211, Saudi Arabia. amarty@kfshrc.edu.sa
authors.forename: J K
authors.initials: JK
authors.lastname: Amartey
authors.forename: C
authors.initials: C
authors.lastname: Esguerra
authors.forename: B
authors.initials: B
authors.lastname: Al-Otaibi
authors.forename: R S
authors.initials: RS
authors.lastname: Parhar
authors.forename: I
authors.initials: I
authors.lastname: Al-Jammaz
mesh_terms: D000818:Animals; D004195:Disease Models, Animal; D004927:Escherichia coli Infections / Q000000981:diagnostic imaging*; D005462:Fluorine Radioisotopes; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis; D007239:Infections / Q000000981:diagnostic imaging*; D007539:Isonicotinic Acids / Q000138:chemical synthesis; D051379:Mice; D008807:Mice, Inbred BALB C; D011877:Radionuclide Imaging; D014397:Tuberculosis, Pulmonary / Q000000981:diagnostic imaging*
chemical_list: C476778:2-fluoroisonicotinic acid hydrazide; D005462:Fluorine Radioisotopes; D006834:Hydrazines; D007539:Isonicotinic Acids