Synthesis of a new series of heterocyclic scaffolds for medicinal purposes.
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.
Hilal
H S
HS
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine. hikmathilal@yahoo.com
Ali-Shtayeh
M S
MS
Arafat
R
R
Al-Tel
T
T
Voelter
W
W
Barakat
A
A
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
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D006571:Heterocyclic Compounds