51891-89-5Relevant articles and documents
Novel N-4-Piperazinyl Ciprofloxacin-Ester Hybrids: Synthesis, Biological Evaluation, and Molecular Docking Studies
Mahdavi, M.,Mostafavi, H.,Shahbazi, A.,Zarrini, G.
, p. 1558 - 1565 (2020/09/21)
Abstract: A series of novel N-4-piperazinylciprofloxacin-ester hybrids has been synthesized and the structures confirmed by1H and 13C NMR, FT-IRspectral data, and elemental analysis. The products have been tested in vitro for their antibacterial activity againstsix bacterial strains (MRSA, Staphylococcusepidermidis, Bacillussubtilis, Escherichia coli,Salmonella enterica, and Klebsiella pneumoniae) and have demonstrated goodantibacterial activity with MIC values range 6.25–200 μg/mL. Antifungal andcytotoxic activities of the products have been tested against Candida kefyr and human leukemia K562 cell line,respectively. All compounds inhibit growth of K562 cells more efficiently thanthe parent ciprofoxacin in a dose- and duration-dependent way. Molecular dockingstudies performed for the compound 3i indicatesthat similarly to ciprofloxacin it can act as an inhibitor of S. aureus DNA gyrase.
ANTI-BIOFILM COMPOUNDS
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Page/Page column 38, (2013/03/26)
The present invention provides non-peptide compounds of formula (I) wherein: X is -(C1-C8)allcyl-, aryl or -aryl(C1-C8)alkyl-; Y is -(C1-C8)alkyl- or absent; W is heteroaryl, (C3-C7)carbocycle or aryl, wherein any heteroaryl, (C3-C7)carbocycle or, aryl of W is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) Z1 groups; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, -CN, NO2, halogen, -ORa, -SRa, -S(O)2NRbRc, -NRbRc, -NRaCORd, -C(O)Ra, -C(O)ORa, and -C(O)NRbRc; R2 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)Jalkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, -CN, NO2, halogen, -ORe, -SRe, -S(O)2NRfRg, -NRfRg -NReCORh, -C(O)Re, -C(O)ORe and -C(O)NRfRg; I that mimic the streptococcal; SspB Adherence Region (BAR) and function as inhibitors of P. gingivalis adherence to streptococci. The invention also provides methods of making and using the inhibitors.