Please use this identifier to cite or link to this item: http://ir.swu.ac.th/jspui/handle/123456789/15021
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
iodouracil
uracil
animal
article
chemical structure
chemistry
drug effect
human
microbiological examination
Moraxella catarrhalis
Neisseria mucosa
Plasmodium falciparum
Streptococcus pyogenes
synthesis
tumor cell line
Animals
Anti-Bacterial Agents
Antimalarials
Cell Line, Tumor
Humans
Microbial Sensitivity Tests
Molecular Structure
Moraxella (Branhamella) catarrhalis
Neisseria mucosa
Plasmodium falciparum
Streptococcus pyogenes
Uracil
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.
URI: https://www.scopus.com/inward/record.uri?eid=2-s2.0-69549121667&doi=10.3390%2fmolecules14082768&partnerID=40&md5=ece40e9bb09084bf4aa78d9d28aaa605
http://ir.swu.ac.th/jspui/handle/123456789/15021
ISSN: 14203049
Appears in Collections:SCOPUS 1983-2021

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