Antimicrobial and antiproliferative activity studies of some new quinoline-3-carbaldehyde hydrazone derivatives
Küçük Resim Yok
Tarih
2020
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Academic Press Inc Elsevier Science
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
In this study, a total of 22 piece quinoline-3-carbaldehyde hydrazone derivative compounds were designed and synthesized, 2 of which were not original, their antimicrobial activities were determined with microdilution method and their in vitro cytotoxic effect was investigated in MCF-7 and A549 cells by MTT assay. When the activity results are examined, although the antimicrobial effects of quinoline derivatives, in general, are weaker than standard drugs; 3q5 and 3q6 against MRSA showed promising activity with MIC:16 mu g/ml compared to reference drugs. Compounds generally showed weaker cytotoxic activity on the A549 and MCF-7 cell line. 3q12, 3q17 and 3q22 at 100 mu M reduced cell viability to 59.28%, 76.24% and 72.92% on A549 cells, respectively. Compound 3q6, one of the most effective compounds against MRSA, formed a 2.10 angstrom long hydrogen bond between the quinoline nitrogen and ARG132 in the DNA topoisomerase IV active site (PDB: 3FV5). Theoretical ADME profiles of all compounds comply with Lipinski and other limiting rules. In addition, MEP analysis of 3q6, geometric optimization and molecular reactivity analysis were calculated with the 6-311G (d,p) base set DFT/ B3LYP theory, and Delta E = ELUMO-EHOMO, which is a measure of the stable structure of the molecule, was cal-culated as 0.13377 for 3q6 and had the most stable electronic structure among all compounds.
Açıklama
Anahtar Kelimeler
Quinoline, Hydrazone, Antimicrobial Activity, Cytotoxicity, Molecular Docking, Spectroscopic Investigations, Thermal-Properties, Complexes, Binding
Kaynak
Bioorganic Chemistry
WoS Q Değeri
Q1
Scopus Q Değeri
Q1
Cilt
101
