849676-07-9Relevant articles and documents
RNA-selective modification by a platinum(II) complex conjugated to amino- and guanidinoglycosides
Boer, Juergen,Blount, Kenneth F.,Luedtke, Nathan W.,Elson-Schwab, Lev,Tor, Yitzhak
, p. 927 - 932 (2005)
Revving up the RNA response: Binding of the anticancer drug cisplatin (cis-Pt) to nucleic acids is believed to favor DNA over RNA. To "reverse" the nucleic acid selectivity of cis-Pt, amino- and guanidinoglycoside-PtII conjugates (1 and 2) have
Use of neomycin as a structured amino-containing side chain motif for phenanthroline-based G-quadruplex ligands and telomerase inhibitors
Singh, Mandeep,Wang, Siwen,Joo, Hyun,Ye, Zhihan,Christison, Krege M.,Hekman, Ryan,Vierra, Craig,Xue, Liang
, p. 1292 - 1304 (2020/07/28)
In this paper, we report the synthesis of a phenanthroline and neomycin conjugate (7). Compound 7 binds to a human telomeric G-quadruplex (G1) with a higher affinity compared with its parent compounds (phenanthroline and neomycin), which is determined by
Synthesis of nucleobase-neomycin conjugates and evaluation of their DNA binding, cytotoxicities, and antibacterial properties
Wang, Siwen,Singh, Mandeep,Ling, Mingheng,Li, Danni,Christison, Krege M.,Lin-Cereghino, Joan,Lin-Cereghino, Geoff P.,Xue, Liang
, p. 1517 - 1527 (2018/04/02)
Neomycin is known to preferentially bind to A-form nucleic acid structures including triplex DNA, DNA and RNA hybrid, and duplex RNA. Tethering a DNA intercalator moiety to the C5” position of the ring III of neomycin is a practical approach to develop po
Aminoglycoside-based novel probes for bacterial diagnostic and therapeutic applications
Zhang, Qingyang,Wang, Qinghua,Xu, Shengnan,Zuo, Limin,You, Xuefu,Hu, Hai-Yu
supporting information, p. 1366 - 1369 (2017/02/05)
Specific detection of pathogens has long been recognized as a vital strategy in the control of infectious diseases. Two novel theranostic neomycin analogs exhibit efficient targeting, labelling and killing of broad spectrum bacteria while not damaging macrophage-like cells. Furthermore, lipidated probe 2 clearly showed antibacterial activity against methicillin-resistant S. aureus.
Arginine-linked neomycin B dimers: Synthesis, rRNA binding, and resistance enzyme activity
Jin, Yi,Watkins, Derrick,Degtyareva, Natalya N.,Green, Keith D.,Spano, Meredith N.,Garneau-Tsodikova, Sylvie,Arya, Dev P.
supporting information, p. 164 - 169 (2016/01/30)
The nucleotides comprising the ribosomal decoding center are highly conserved, as they are important for maintaining translational fidelity. The bacterial A-site has a small base variation as compared with the human analogue, allowing aminoglycoside (AG) antibiotics to selectively bind within this region of the ribosome and negatively affect microbial protein synthesis. Here, by using a fluorescence displacement screening assay, we demonstrate that neomycin B (NEO) dimers connected by l-arginine-containing linkers of varying length and composition bind with higher affinity to model A-site RNAs compared to NEO, with IC50 values ranging from ~40-70 nM, and that a certain range of linker lengths demonstrates a clear preference for the bacterial A-site RNA over the human analogue. Furthermore, AG-modifying enzymes (AMEs), such as AG O-phosphotransferases, which are responsible for conferring antibiotic resistance in many types of infectious bacteria, demonstrate markedly reduced activity against several of the l-arginine-linked NEO dimers in vitro. The antimicrobial activity of these dimers against several bacterial strains is weaker than that of the parent NEO.
Methods and compositions related to viral inhibition
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Page/Page column 88; 89; 105; 106; 109; 110, (2015/07/15)
Disclosed herein are compounds, compositions and methods related to viral inhibition. In some forms, the compounds, compositions and methods are related to binding RNA.
Rapid synthesis, RNA binding, and antibacterial screening of a peptidic-aminosugar (PA) library
Jiang, Liuwei,Watkins, Derrick,Jin, Yi,Gong, Changjun,King, Ada,Washington, Arren Z.,Green, Keith D.,Garneau-Tsodikova, Sylvie,Oyelere, Adegboyega K.,Arya, Dev P.
, p. 1278 - 1289 (2015/06/02)
A 215-member mono- and diamino acid peptidic-aminosugar (PA) library, with neomycin as the model aminosugar, was systematically and rapidly synthesized via solid phase synthesis. Antibacterial activities of the PA library, on 13 bacterial strains (seven G
Neomycin-phenolic conjugates: Polycationic amphiphiles with broad-spectrum antibacterial activity, low hemolytic activity and weak serum protein binding
Findlay, Brandon,Zhanel, George G.,Schweizer, Frank
, p. 1499 - 1503 (2012/04/04)
Here we present a proof-of-concept study, combining two known antimicrobial agents into a hybrid structure in order to develop an emergent cationic detergent-like interaction with the bacterial membrane. Six amphiphilic conjugates were prepared by copper
Click dimers to target HIV TAR RNA conformation
Kumar, Sunil,Kellish, Patrick,Robinson, W. Edward,Wang, Deyun,Appella, Daniel H.,Arya, Dev P.
scheme or table, p. 2331 - 2347 (2012/06/29)
A series of neomycin dimers have been synthesized using "click chemistry" with varying functionality and length in the linker region to target the human immunodeficiency virus type 1 (HIV-1) TAR RNA region of the HIV virus. The TAR (Trans-Activation Respo
HYDROPHOBICALLY ENHANCED AMINOGLYCOSIDES
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Page/Page column 19-20, (2011/08/04)
Hydrophobically enhanced aminoglycosides have been prepared and shown to be effective antibacterial agents. These agents may be used in the treatment or prevention of various bacterial infections. Methods of preparing these agents also permit facile synth
