Syntheses and biological activity of some derivatives of C-9154 antibiotic.
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.
Department of Chemistry, Ahmadu Bello University, Zaria 810001, Nigeria.
Isaac Asusheyi
IA
Bello
Department of Chemistry, Ahmadu Bello University, Zaria 810001, Nigeria.
George Iloegbulam
GI
Ndukwe
Department of Chemistry, Ahmadu Bello University, Zaria 810001, Nigeria.
Joseph Olorunju
JO
Amupitan
Division of Agricultural Colleges, College of Agriculture, Ahmadu Bello University, Zaria 810001, Nigeria.
Rachael Gbekele
RG
Ayo
School of Chemistry and Biochemistry, University of Zululand, Empangeni 3880, South Africa.
Francis Oluwole
FO
Shode