55580-07-9Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 3-amino-2-oxazolidinone derivatives as potent quorum-sensing inhibitors of Pseudomonas aeruginosa PAO1
Jiang, Kai,Lin, Feng,Wu, Hao,Xiao, Junhai,Xiao, Zijian,Yan, Xinlin,Yu, Jiahao,Yue, Yuandong,Zhao, Meihua,Zhou, Xiaoping
, (2020/03/31)
Due to the increasing resistance of Pseudomonas aeruginosa to most clinically relevant antimicrobials, it is challenging to treat bacterial infection with traditional antibiotics. Quorum sensing can regulate the production of biofilms and virulence factors which are closely related to bacterial resistance. Previously we synthesized a series of oxazolidinone compounds targeting the quorum-sensing transcriptional regulatory protein CviR and ZS-12 showed good activity against Chromobacterium violaceum CV026 quorum-sensing. In this study, eighteen 3-amino-2-oxazolidinone compounds were designed and synthesized using ZS-12 as the lead compound. We initially evaluated the inhibitory activities of novel oxazolidinone compounds against QS using C. violaceum CV026 as a reporter strain. Thirteen compounds showed good activities (IC50 range 3.69–63.58 μM) and YXL-13 inhibition was the most significant (IC50 = 3.686 ± 0.5790 μM) against biofilm formation and virulence factors determination of P. aeruginosa PAO1. In vitro, YXL-13 significantly inhibited the formation of PAO1 biofilm (range 42.98%–17.67%), the production of virulence factors (pyocyanin, elastase, rhamnolipid, and protease), and bacterial motility. Moreover, the combination of YXL-13 with an antibiotic (meropenem trihydrate) could significantly improve the antibiotic susceptibility of biofilm P. aeruginosa PAO1 cells. In vivo, YXL-13 significantly prolonged the lifespan of wildtype Caenorhabditis elegans N2 infected by P. aeruginosa PAO1. In conclusion, YXL-13 is a candidate agent for antibiotic-resistant P. aeruginosa PAO1and provides a method for finding new antibacterial drugs.
Acene-based transmitter molecules for photon upconversion
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Paragraph 0144; 0145, (2018/10/04)
Provided herein are transmitter ligands that improve photon upconversion of near infrared light (NIR) to visible light. The presently provided ligands are complexed to semiconductor nanocrystals and improve triplet energy transfer from semiconductor nanocrystal to annihilator in triplet-triplet annihilation. Suitable applications include bio-imaging.
SUBSTITUTED POLYCYCLIC ANTIBACTERIAL COMPOUNDS
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Page/Page column 150; 151, (2016/02/29)
The present description relates to substituted polycyclic compounds of Formula (I), Formula (II) or Formula (III): wherein the dashed line represents an optional double bond and Rl, R2, R4, R5, R7, X and Z are as defined herein, and forms and compositions thereof, and also relates to uses of a compound of Formula (I), Formula (II) or Formula (III) or a form thereof and methods for treating or ameliorating Neisseria gonorrhoeae (N. gonorrhoeae) in a subject in need thereof comprising, administering an effective amount of the compound to the subject.
Catalytic Access to Alkyl Bromides, Chlorides and Iodides via Visible Light-Promoted Decarboxylative Halogenation
Candish, Lisa,Standley, Eric A.,Gómez-Suárez, Adrián,Mukherjee, Satobhisha,Glorius, Frank
supporting information, p. 9971 - 9974 (2016/07/19)
Herein is reported the catalytic, visible light-promoted, decarboxylative halogenation (bromination, chlorination, and iodination) of aliphatic carboxylic acids. This operationally-simple reaction tolerates a range of functional groups, proceeds at room temperature, and is redox neutral. By employing an iridium photocatalyst in concert with a halogen atom source, the use of stoichiometric metals such as silver, mercury, thallium, and lead can be circumvented. This reaction grants access to valuable synthetic building blocks from the large pool of cheap, readily available carboxylic acids.
Potent inhibitors of LpxC for the treatment of gram-negative infections
Brown, Matthew F.,Reilly, Usa,Abramite, Joseph A.,Arcari, Joel T.,Oliver, Robert,Barham, Rose A.,Che, Ye,Chen, Jinshan Michael,Collantes, Elizabeth M.,Chung, Seung Won,Desbonnet, Charlene,Doty, Jonathan,Doroski, Matthew,Engtrakul, Juntyma J.,Harris, Thomas M.,Huband, Michael,Knafels, John D.,Leach, Karen L.,Liu, Shenping,Marfat, Anthony,Marra, Andrea,McElroy, Eric,Melnick, Michael,Menard, Carol A.,Montgomery, Justin I.,Mullins, Lisa,Noe, Mark. C.,O'Donnell, John,Penzien, Joseph,Plummer, Mark S.,Price, Loren M.,Shanmugasundaram, Veerabahu,Thoma, Christy,Uccello, Daniel P.,Warmus, Joseph S.,Wishka, Donn G.
supporting information; experimental part, p. 914 - 923 (2012/03/27)
In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid 1a.
OXAZOLIDINONE DERIVATIVES N-SUBSTITUTED BY A BICYCLIC RING, FOR USE AS ANTIBACTERIAL AGENTS
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Page/Page column 94, (2010/02/08)
Compounds of formula (I) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compoun
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: Synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety
Shiraishi, Mitsuru,Aramaki, Yoshio,Seto, Masaki,Imoto, Hiroshi,Nishikawa, Youichi,Kanzaki, Naoyuki,Okamoto, Mika,Sawada, Hidekazu,Nishimura, Osamu,Baba, Masanori,Fujino, Masahiko
, p. 2049 - 2063 (2007/10/03)
The search for new small-molecule CCR5 antagonists by high-throughput screening (HTS) of the Takeda chemical library using [125I]RANTES and CHO/CCR5 cells led to the discovery of lead compounds (A, B) with a quaternary ammonium or phosphonium m
