| Content Provider |
World Health Organization (WHO)-Global Index Medicus |
| Author |
El-Awdan, S. A. El-Sherif, A. A. Moahamed, Y. A. Salem, M. A. Abd-elaziz, T. A. Mohamed, G. A. M. Helal, M. H. |
| Description |
Country affiliation: Saudi Arabia Author Affiliation: Helal MH ( Department of Chemistry, Faculty of Science, Al-Azhar University, 11284 Nasr City, Cairo, Egypt); El-Awdan SA ( Pharmacology Department, National Research Center, El-Bohoth St., Dokki, P.O. 12622, Cairo, Egypt.); Salem MA ( Department of Chemistry, Faculty of Science, Al-Azhar University, 11284 Nasr City, Cairo, Egypt); Abd-elaziz TA ( Department of Chemistry, Faculty of Science, Al-Azhar University, 11284 Nasr City, Cairo, Egypt.); Moahamed YA ( Department of Chemistry, Faculty of Science, Al-Azhar University, 11284 Nasr City, Cairo, Egypt.); El-Sherif AA ( Department of Chemistry, Faculty of Arts and Science, Northern Border University, Rafha, Saudi Arabia); Mohamed GA ( Department of Chemistry, Faculty of Science, Al-Azhar University, 11284 Nasr City, Cairo, Egypt.) |
| Abstract |
This paper presents a combined synthesis; characterization, computational and biological activity studies of novel series of pyridines heterocyclic compounds. The compounds have been characterized by elemental analyses and spectral like IR, (1)H NMR, (13)C NMR and MS studies. Michael addition of substituted-2-methoxycarbonylacetanilide 2a,b on the -substituted cinnamonitriles 3a-d gave the corresponding 2-pyridone derivatives 5-10. Structures of the titled compounds cited in this article were elucidated by spectrometric data (IR, (1)H NMR, (13)C NMR and MS). The molecular modeling of the synthesized compounds has been drawn and their molecular parameters were calculated. Also, valuable information is obtained from the calculation of molecular parameters including electronegativity, net dipole moment of the compounds, total energy, electronic energy, binding energy, HOMO and LUMO energy. Various in vitro antitumor as well as in vivo anti-inflammatory and analgesic activities of the synthesized compounds were investigated. Evaluation of anti-inflammatory activity of test compounds was performed using carrageenan induced paw edema in rats. All the tested compounds showed moderate to good activity. The SAR results indicate that all compounds showed moderate to good activity, among these 7 and 10 compounds having -N(CH3)2 group are most effective. |
| ISSN |
13861425 |
| Volume Number |
135 |
| e-ISSN |
18733557 |
| Journal |
Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy |
| Language |
English |
| Publisher |
Elsevier |
| Publisher Date |
2015-01-25 |
| Publisher Place |
Great Britain (UK) |
| Access Restriction |
One Nation One Subscription (ONOS) |
| Subject Keyword |
Analgesics Pharmacology Anti-inflammatory Agents Antineoplastic Agents Models, Molecular Pyridines Chemical Synthesis Chemistry Animals Cell Death Drug Effects Female Hep G2 Cells Humans Male Molecular Conformation Rats Structure-activity Relationship Journal Article Discipline Spectroscopy |
| Content Type |
Text |
| Resource Type |
Article |
| Subject |
Spectroscopy Atomic and Molecular Physics, and Optics Analytical Chemistry Instrumentation |
