Synthesis, Biocidal and Antibiofilm Activities of New Isatin-Quinoline Conjugates against Multidrug-Resistant Bacterial Pathogens along with Their In Silico Screening.

Autor:	Elmongy EI; Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia., Ahmed AAS; Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Kom 32511, Egypt., El Sayed IET; Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Kom 32511, Egypt., Fathy G; Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Kom 32511, Egypt., Awad HM; Department of Tanning Materials and Leather Technology, National Research Centre, Dokki, Giza 12611, Egypt., Salman AU; Department of Botany and Microbiology, Faculty of Science, Menoufia University, Shebin El-Kom 32511, Egypt., Hamed MA; Chemistry Department, Faculty of Science, Tanta University, Tanta 31511, Egypt.
Jazyk:	angličtina
Zdroj:	Antibiotics (Basel, Switzerland) [Antibiotics (Basel)] 2022 Oct 28; Vol. 11 (11). Date of Electronic Publication: 2022 Oct 28.
DOI:	10.3390/antibiotics11111507
Abstrakt:	Isatin-quinoline conjugates 10a - f and 11a - f were assembled by the reaction of N-(bromobutyl) isatin derivatives 3a , b with aminoquinolines 6a - c and their corresponding hydrazinyl 9a - c in good yields. The structures of the resulting conjugates were established by spectroscopic tools and showed data consistent with the proposed structures. In vitro antibacterial activity against different bacterial strains was evaluated. All tested conjugates showed significant biocidal activity with lower MIC than the first line drugs chloramphenicol and ampicillin. Conjugates 10a , 10b and 10f displayed the most potent activity against all clinical isolates. The antibiofilm activity for all tested conjugates was screened against the reference drug vancomycin using the MRSA strain. The results revealed that all conjugates had an inhibitory activity against biofilm formation and conjugate. Conjugate 11a showed 83.60% inhibition at 10 mg/mL. In addition, TEM studies were used to prove the mechanism of antibacterial action of conjugates 10a and 11a against ( MRSA ). Modeling procedures were performed on 10a - f and 11a - f and interestingly the results were nearly consistent with the biological activities. In addition, in silico pharmacokinetic evaluation was performed and revealed that the synthesized compounds 10a - f and 11a - f were considered drug-like molecules with promising bioavailability and high GI absorption. The results confirmed that the title compounds caused the disruption of bacterial cell membranes and could be used as potential leads for the further development and optimization of antibacterial agents.
Databáze:	MEDLINE
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