1093192-07-4Relevant academic research and scientific papers
COMPOUND ACTING AS ANTIBIOTICS
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, (2020/12/22)
The present invention provides a novel antibiotic compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, an ester thereof, a prodrug thereof, a solvate thereof, or a deuterated analog thereof, or a stereoisomer thereof. The compound of the present invention exhibits excellent antibacterial activity, especially against Gram bacteria. wherein each group is defined as in the description.
Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents
Ding, Shi,Dai, Rui-Yang,Wang, Wen-Ke,Cao, Qiao,Lan, Le-Fu,Zhou, Xian-Li,Yang, Yu-She
, p. 94 - 102 (2017/12/15)
LpxC inhibitors are new-type antibacterial agents developed in the last twenty years, mainly against Gram-negative bacteria infections. To develop novel LpxC inhibitors with good antibacterial activities and biological metabolism, we summarized the basic skeleton of reported LpxC inhibitors, designed and synthesized several series of compounds and tested their antibacterial activities against Escherichial coli and Pseudomonas aeruginosa in vitro. Structure-activity relationships have been discussed in this article. The metabolism stability of YDL-2, YDL-5, YDL-8, YDL-14, YDL-20–YDL-23 have been evaluated in liver microsomes, which indicated that the 2-amino isopropyl group may be a preferred structure than the 2-hydroxy ethyl group in the design of LpxC inhibitors.
Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC
Piizzi, Grazia,Parker, David T.,Peng, Yunshan,Dobler, Markus,Patnaik, Anup,Wattanasin, Som,Liu, Eugene,Lenoir, Francois,Nunez, Jill,Kerrigan, John,McKenney, David,Osborne, Colin,Yu, Donghui,Lanieri, Leanne,Bojkovic, Jade,Dzink-Fox, Joann,Lilly, Maria-Dawn,Sprague, Elizabeth R.,Lu, Yipin,Wang, Hongming,Ranjitkar, Srijan,Xie, Lili,Wang, Bing,Glick, Meir,Hamann, Lawrence G.,Tommasi, Ruben,Yang, Xia,Dean, Charles R.
, p. 5002 - 5014 (2017/06/28)
Over the past several decades, the frequency of antibacterial resistance in hospitals, including multidrug resistance (MDR) and its association with serious infectious diseases, has increased at alarming rates. Pseudomonas aeruginosa is a leading cause of nosocomial infections, and resistance to virtually all approved antibacterial agents is emerging in this pathogen. To address the need for new agents to treat MDR P. aeruginosa, we focused on inhibiting the first committed step in the biosynthesis of lipid A, the deacetylation of uridyldiphospho-3-O-(R-hydroxydecanoyl)-N-Acetylglucosamine by the enzyme LpxC. We approached this through the design, synthesis, and biological evaluation of novel hydroxamic acid LpxC inhibitors, exemplified by 1, where cytotoxicity against mammalian cell lines was reduced, solubility and plasma-protein binding were improved while retaining potent anti-pseudomonal activity in vitro and in vivo.
ANTIBACTERIAL AGENTS
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Page/Page column 42; 43, (2014/10/18)
Antibacterial compounds of formula (I) are provided, as well as stereoisomers and pharmaceutically acceptable salts and esters thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
ETHYNYLBENZENE DERIVATIVES
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, (2012/03/26)
Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
ORGANIC COMPOUNDS FOR APPLICATIONS IN BACTERIAL INFECTIONS TREATMENT
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Page/Page column 70, (2010/04/25)
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
ANTIBACTERIAL AGENTS
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, (2009/01/24)
Antibacterial compounds of formula (I) are provided, as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
