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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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Hilal HS,Ali-Shtayeh MS,Arafat R,Al-Tel T,Voelter W,Barakat A

doi

10.1016/j.ejmech.2006.03.025

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

1017-24

issue

8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(06)00138-3

journal_volume

41

pub_type

杂志文章

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