Publication: Synthesis, antioxidant and antimicrobial activities of metal complexes of 2-thiouracil-hydroxyquinoline derivatives
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Issued Date
2018
Resource Type
File Type
application/pdf
ISSN
15701808
Other identifier(s)
2-s2.0-85047833262
Rights Holder(s)
Scopus
Bibliographic Citation
Letters in Drug Design and Discovery. Vol 15, No.6 (2018), p.602-611
Suggested Citation
Worachartcheewan A., Pingaew R., Lekcharoen D., Prachayasittikul S., Ruchirawat S., Prachayasittikul V. Synthesis, antioxidant and antimicrobial activities of metal complexes of 2-thiouracil-hydroxyquinoline derivatives. Letters in Drug Design and Discovery. Vol 15, No.6 (2018), p.602-611. doi:10.2174/1570180814666170922163828 Retrieved from: https://hdl.handle.net/20.500.14740/3953
Abstract
Introduction: Metal ions are cofactors found in antioxidant enzymes such as superoxide dismutase (SOD), and are essential in catalytic mechanisms for scavenging the free radicals. Therefore, synthetic compounds containing metal ions coordination are designed for SOD mimic and other biological activities. Objective: This study aimed to synthesize metal (Ni, Cu, Mn) complexes of mixed ligands of 2-thiouracil (2TU) with 8-hydroxyquinoline (8HQ) (1-3) and with 2-hydroxyquinoline (2HQ) (4-6), and to determine antioxidant and antimicrobial activities. Results: The metal complexes 1-6 elicited SOD activity with IC50 of 1.20-500.26 µM, particularly, complex 5 (2TU-Cu-2HQ) showed the highest SOD activity with IC50 of 1.20 µM. In addition, complexes 1 (2TU-Ni-8HQ), 5 and 2 (2TU-Cu-8HQ) displayed radical scavenging activity (RSA) with IC50 of 174.86, 196.54 and 431.65 µM, respectively, whereas the complexes 3, 4 and 6 were shown to be inactive. Furthermore, the metal complex 3 (2TU-Mn-8HQ) exhibited good antimicrobial activity with the minimal inhibitory concentration (MIC) range of 11.07-708.64 µM against gram positive and gram negative bacteria as well as diploid fungus, followed by metal complexes 2 (MIC of 23.68-757.70 µM) and 1 (MIC of 350.67-701.35 µM). Interestingly, among the similar mixed ligands with different metal ions of complexes 1 (Ni), 2 (Cu) and 3 (Mn), the complex 3 has the highest SOD (IC50 = 3.50 µM) and antimicrobial activities, but Cu complex (5) of 2TU and 2HQ showed higher SOD and RSA activities than Ni (4) and Mn (6) complexes. Conclusion: This finding reveals novel transition metal complexes with a potential for further development as medicinal compounds. © 2018 Bentham Science Publishers.
Subject(s)
8 quinolinol derivative
Ampicillin
Antiinfective agent
Antioxidant
Copper complex
Manganese complex
Metal complex
Metal ion
Nickel complex
Quinolinol derivative
Superoxide dismutase
Thiouracil derivative
Unclassified drug
Agar dilution
Antimicrobial activity
Antioxidant activity
Article
Chemical bond
Controlled study
DPPH radical scavenging assay
Drug synthesis
Enzyme activity
Enzyme assay
Fungus
Gram negative bacterium
Gram positive bacterium
IC50
Magnetic field
Mass spectrometry
Minimum inhibitory concentration
Nonhuman
Priority journal
Ampicillin
Antiinfective agent
Antioxidant
Copper complex
Manganese complex
Metal complex
Metal ion
Nickel complex
Quinolinol derivative
Superoxide dismutase
Thiouracil derivative
Unclassified drug
Agar dilution
Antimicrobial activity
Antioxidant activity
Article
Chemical bond
Controlled study
DPPH radical scavenging assay
Drug synthesis
Enzyme activity
Enzyme assay
Fungus
Gram negative bacterium
Gram positive bacterium
IC50
Magnetic field
Mass spectrometry
Minimum inhibitory concentration
Nonhuman
Priority journal