Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives
Joint Authors
Ghabbour, Hazem A.
Barakat, Assem
Yousuf, Sammer
Al-Majid, A. M. A.
Qurat-ul-ain, Abdullah Mohammed
Imad, Rehan
Javaid, Kulsoom
Shaikh, Nimra Naveed
Iqbal Choudhary, M.
Wadood, Abdul
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-05-11
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
A series of barbiturates derivatives synthesized and screened for different set of bioassays are described.
The molecular structures of compounds 5a, 5d, and 5f were solved by single-crystal X-ray diffraction techniques.
The results of bioassay show that compounds 4a, 4b, 4c, 4d, 4e, 4f, and 4g are potent antioxidants in comparison to the tested standards, butylated hydroxytoluene (BHT), and N -acetylcysteine.
Compounds 4a–4e ( I C 50 = 101.8 ± 0.8 – 124.4 ± 4.4 μ M ) and 4g ( I C 50 = 104.1 ± 1.9 μ M ) were more potent antioxidants than the standard (BHT, I C 50 = 128.8 ± 2.1 μ M ).
The enzyme inhibition potential of these compounds was also evaluated, in vitro, against thymidine phosphorylase, α -glucosidase, and β -glucuronidase enzymes.
Compounds 4c, 4h, 4 o , 4p, 4q, 5f, and 5m were found to be potent α -glucosidase inhibitors and showed more activity than the standard drug acarbose, whereas compounds 4v, and 5h were found to be potent thymidine phosphorylase inhibitors, more active than the standard drug, 7-deazaxanthine.
All barbiturates derivatives (4a–4x, 4z, and 5a–5m) were found to be noncytotoxic against human prostate (PC-3), Henrietta Lacks cervical (HeLa) and Michigan Cancer Foundation-7 breast (MCF-7) cancer cell lines, and 3T3 normal fibroblast cell line, except 4y which was cytotoxic against all the cell lines.
American Psychological Association (APA)
Barakat, Assem& Ghabbour, Hazem A.& Al-Majid, A. M. A.& Qurat-ul-ain, Abdullah Mohammed& Imad, Rehan& Javaid, Kulsoom…[et al.]. 2016. Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives. Journal of Chemistry،Vol. 2016, no. 2016, pp.1-11.
https://search.emarefa.net/detail/BIM-1107783
Modern Language Association (MLA)
Barakat, Assem…[et al.]. Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives. Journal of Chemistry No. 2016 (2016), pp.1-11.
https://search.emarefa.net/detail/BIM-1107783
American Medical Association (AMA)
Barakat, Assem& Ghabbour, Hazem A.& Al-Majid, A. M. A.& Qurat-ul-ain, Abdullah Mohammed& Imad, Rehan& Javaid, Kulsoom…[et al.]. Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives. Journal of Chemistry. 2016. Vol. 2016, no. 2016, pp.1-11.
https://search.emarefa.net/detail/BIM-1107783
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1107783