title: Synthesis of a new series of heterocyclic scaffolds for medicinal purposes.
abstract: A new series of substituted 8-fluro-4H-pyrimido[2,1-b] [1,3]benzothiazole-4-ones () substituted 7-methyl-4H-isoxazolo[2,3-a]pyrimidin-4-ones, and substituted 2-methyl-5,6,7,8-tetrahydro-9H-isoxazolo[2,3-a]pyridopyrimidin-9-ones, compounds I-VII, have been prepared via condensation of beta-keto esters with 2-aminopyridine derivatives, in the presence of polyphosphoric acid. The same technique has also been used to prepare diazepine compounds, VIII-X, by condensation of a gamma-keto ester with 2-aminopyridine derivatives. Details of synthetic procedures are shown. The new compounds have been characterized by elemental analysis, GC-MS, FT-IR and NMR spectrometry. Antibacterial, antifungal and anticancer (cytotoxic) activities, for three of these compounds, have been investigated and are presented.
authors.affiliation: College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine. hikmathilal@yahoo.com
authors.forename: H S
authors.initials: HS
authors.lastname: Hilal
authors.forename: M S
authors.initials: MS
authors.lastname: Ali-Shtayeh
authors.forename: R
authors.initials: R
authors.lastname: Arafat
authors.forename: T
authors.initials: T
authors.lastname: Al-Tel
authors.forename: W
authors.initials: W
authors.lastname: Voelter
authors.forename: A
authors.initials: A
authors.lastname: Barakat
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D008401:Gas Chromatography-Mass Spectrometry; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D006571:Heterocyclic Compounds