Please use this identifier to cite or link to this item:
Title: Synthesis of N-substituted 5-iodouracils as antimicrobial and anticancer agents
Authors: Prachayasittikul S.
Sornsongkhram N.
Pingaew R.
Worachartcheewan A.
Ruchirawat S.
Prachayasittikul V.
Keywords: 5-iodouracil
antiinfective agent
antimalarial agent
drug derivative
chemical structure
drug effect
microbiological examination
Moraxella catarrhalis
Neisseria mucosa
Plasmodium falciparum
Streptococcus pyogenes
tumor cell line
Anti-Bacterial Agents
Cell Line, Tumor
Microbial Sensitivity Tests
Molecular Structure
Moraxella (Branhamella) catarrhalis
Neisseria mucosa
Plasmodium falciparum
Streptococcus pyogenes
Issue Date: 2009
Abstract: This study reports the synthesis of some substituted 5-iodouracils and their bioactivities. Alkylation of 5-iodouracils gave predominately N1-substituted-(R)-5-iodouracil compounds 7a-d (R = n-C4H 9, s-C4H9, CH2C6H 11, CH2C6H5) together with N1,N3-disubstituted (R) analogs 8a-b (R = n-C4H9, CH2C6H11). Their antimicrobial activity was tested against 27 strains of microorganisms using the agar dilution method. The analogs 7a, 7c and 7d displayed 25-50% inhibition against Branhamella catarrhalis, Neisseria mucosa and Streptococcus pyogenes at 0.128 mg/mL. No antimalarial activity was detected for any of the analogs when tested against Plasmodium falciparum (T9.94). Their anticancer activity was also examined. Cyclohexylmethyl analogs 7c and 8b inhibited the growth of HepG2 cells. Significantly, N1,N3-dicyclohexylmethyl analog 8b displayed the most potent anticancer activity, with an IC50 of 16.5 ?g/mL. These 5-iodouracil analogs represent a new group of anticancer and antibacterial agents with potential for development for medicinal applications.
ISSN: 14203049
Appears in Collections:SCOPUS 1983-2021

Files in This Item:
There are no files associated with this item.

Items in SWU repository are protected by copyright, with all rights reserved, unless otherwise indicated.