Diazepine

MSShtayeh's picture

Synthesis of a New Series of Heterocyclic Scaffolds for Medicinal Purposes

Journal Title, Volume, Page: 
European Journal of Medicinal Chemistry Volume 41, Issue 8, August 2006, Pages 1017–1024
Year of Publication: 
2006
Authors: 
H.S. Hilal
Faculty of Science, An-Najah National University, Nablus. Palestine
M.S. Ali-Shtayeh
Faculty of Science, An-Najah National University, Nablus. Palestine
Current Affiliation: 
Department of Biology and Biotechnology, Faculty of Science, An-Najah National University, Nablus. Palestine
R. Arafat
Faculty of Science, An-Najah National University, Nablus. Palestine
T. Al-Tel
Faculty of Science, An-Najah National University, Nablus. Palestine
W. Voelter
Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany
A. Barakat
Faculty of Science, An-Najah National University, Nablus. Palestine
Preferred Abstract (Original): 

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 β-keto esters with 2-aminopyridine derivatives, in the presence of polyphosphoric acid. The same technique has also been used to prepare diazepine compounds, VIIIX, by condensation of a γ-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.

adhamtaha's picture

Synthesis and Antibacterial Activity of Novel Curcumin Derivatives Containing Heterocyclic Moiety

Journal Title, Volume, Page: 
Iran J Pharm Res., 12(1): 47–56
Year of Publication: 
2013
Authors: 
Adham Abu Taha
Department of Chemistry, An-Najah National University, Nablus, Palestine
Current Affiliation: 
Faculty of Medicine & Health Sciences, Department of Biomedical Sciences, An-Najah National University, Nablus, Palestine
Noha Mehdawi
Department of Chemistry, An-Najah National University, Nablus, Palestine
Othman A. Hamed
Department of Chemistry, An-Najah National University, Nablus, Palestine
Emad M. Hamed
Department of Chemistry, Hashemite University, Zarqa, Jordan
Mohammed A. Al-Nuri
Department of Chemistry, An-Najah National University, Nablus, Palestine
Ayman S. Hussein
College of Pharmacy, Genetics Laboratory, An-Najah National University, Nablus, Palestine
Preferred Abstract (Original): 

A series of curcumin derivatives containing heterocyclic moiety have been synthesized and evaluated for their antibacterial activities. The chemical structures of the synthesized compounds were verified on the basis of spectral data and elemental analyses. Investigation of antimicrobial activity of the derivatives demonstrated the ability to inhibit Gram-positive microorganisms with zone of inhibition ranging from 14-18 mm, MIC ranging between 0.0625 and 0.25 mg/mL. Among all tested derivatives, diazepine 4 exhibited remarkable potency against Gram-positive bacteria S. aureus. An extensive study is underway to optimize the effectiveness of diazepine type of compounds and to determine their mode of action.

2038's picture

Synthesis of a New Saries of Hetrocyclic Scaffolds for Medicinal Purposes

Journal Title, Volume, Page: 
European Journal of Medicinal Chemistry.
Year of Publication: 
2006
Authors: 
A. Barakat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
Current Affiliation: 
Department of Statistics, An-Najah National University, Nablus, Palestine
Hikmat, S. H.
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
M.S. Ali-Shtayeh
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
R. Arafat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
T. Al-Tel
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
W. Voelter
Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany
Preferred Abstract (Original): 

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 β-keto esters with 2-aminopyridine derivatives, in the presence of polyphosphoric acid. The same technique has also been used to prepare diazepine compounds, VIIIX, by condensation of a γ-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.

2473's picture

Synthesis and Antibacterial Activity of Novel Curcumin Derivatives Containing Heterocyclic Moiety

Journal Title, Volume, Page: 
Iranian Journal of Pharmaceutical Research (2013), 12 (1):47-56
Year of Publication: 
2013
Authors: 
Othman A. Hamed
Department of Chemistry, An-Najah National University, Nablus, Palestine
Current Affiliation: 
Department of Chemistry, An-Najah National University, Nablus, Palestine
Noha Mehdawi
Department of Chemistry, An-Najah National University, Nablus, Palestine
Adham Abu Taha
College of Pharmacy, Genetics Laboratory, An-Najah National University, Nablus, Palestine
Emad M. Hamed
Department of Chemistry, Hashemite University, Zarqa, Jordan
Mohammed A. Al-Nuri
Department of Chemistry, An-Najah National University, Nablus, Palestine
Ayman S. Hussein
College of Pharmacy, Genetics Laboratory, An-Najah National University, Nablus, Palestine
Preferred Abstract (Original): 

A series of curcumin derivatives containing heterocyclic moiety have been synthesized and evaluated for their antibacterial activities. The chemical structures of the synthesized compounds were verified on the basis of spectral data and elemental analyses. Investigation of antimicrobial activity of the derivatives demonstrated the ability to inhibit Gram-positive microorganisms with zone of inhibition ranging from 14-18 mm, MIC ranging between 0.0625 and 0.25 mg/mL. Among all tested derivatives, diazepine 4 exhibited remarkable potency against Gram-positive bacteria S. aureus. An extensive study is underway to optimize the effectiveness of diazepine type of compounds and to determine their mode of action.

Hikmat S. Hilal's picture

Synthesis of a New Series of Heterocyclic Scaffolds for Medicinal Purposes

Journal Title, Volume, Page: 
European Journal of Medicinal Chemistry Volume 41, Issue 8, August 2006, Pages 1017-1024
Year of Publication: 
2006
Authors: 
H.S. Hilal
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
Current Affiliation: 
Department of Chemistry, An-Najah N. University, Nablus, PO Box 7, West Bank, Palestine
M.S. Ali-Shtayeh
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
R. Arafat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
T. Al-Tel
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
W. Voelter
Abteilung für Physikalische Biochemie des Physiologisch-Chemischen Instituts der Universität Tübingen, Hoppe-Seyler Straße 4, 72076 Tübingen, Germany
A. Barakat
College of Sciences, An-Najah N. University, PO Box 7, Nablus, Palestine
Preferred Abstract (Original): 

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 β-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 γ-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.

Synthesis of a new series of heterocyclic scaffolds for medicinal purposes

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