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Syntheses and Biological Activity of Some Derivatives of C-9154 Antibiotic
Joint Authors
Amupitan, Joseph Olorunju
Bello, Isaac Asusheyi
Ayo, Rachael Gbekele
Ndukwe, George Iloegbulam
Shode, Francis Oluwole
Source
International Journal of Medicinal Chemistry
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-08-07
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Abstract EN
This research was undertaken to design several new antibiotics, by structurally modifying the C-9154 antibiotic, simultaneously improving its activity and lowering toxicity.
This was achieved by synthesizing an analogue to the C-9154 antibiotic and seven derivatives of this analogue.
The approach was to significantly reduce the polarity of the synthesized analogue in the derivatives to achieve increased permeability across cell membranes by conversion of the highly polar carboxylic group to an ester functional group.
The compounds were fully characterized using infrared, GC-MS, and 1D and 2D NMR experiments.
The in vitro biological activity of the compounds showed that the derivatives were more active than the analogue as was anticipated and both were more active than the standard drugs used for comparison.
Work is ongoing to establish applications for the compounds as antiplasmodials, antivirals, anticancers/tumours, antitrypanosomiasis, anthelminthic, and as general antibiotics for human, veterinary, and even agricultural use as they had marked effect on both Gram-positive and Gram-negative bacteria and some fungi.
American Psychological Association (APA)
Bello, Isaac Asusheyi& Ndukwe, George Iloegbulam& Amupitan, Joseph Olorunju& Ayo, Rachael Gbekele& Shode, Francis Oluwole. 2012. Syntheses and Biological Activity of Some Derivatives of C-9154 Antibiotic. International Journal of Medicinal Chemistry،Vol. 2012, no. 2012, pp.1-7.
https://search.emarefa.net/detail/BIM-449583
Modern Language Association (MLA)
Bello, Isaac Asusheyi…[et al.]. Syntheses and Biological Activity of Some Derivatives of C-9154 Antibiotic. International Journal of Medicinal Chemistry No. 2012 (2012), pp.1-7.
https://search.emarefa.net/detail/BIM-449583
American Medical Association (AMA)
Bello, Isaac Asusheyi& Ndukwe, George Iloegbulam& Amupitan, Joseph Olorunju& Ayo, Rachael Gbekele& Shode, Francis Oluwole. Syntheses and Biological Activity of Some Derivatives of C-9154 Antibiotic. International Journal of Medicinal Chemistry. 2012. Vol. 2012, no. 2012, pp.1-7.
https://search.emarefa.net/detail/BIM-449583
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-449583