728877-98-3Relevant academic research and scientific papers
NOVEL COMPOUNDS AND THEIR USE
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Page/Page column 76-78, (2021/06/26)
The present invention provides compounds of the general formula (I) or a pharmaceutically acceptable prodrugs, salts and/or solvates thereof, wherein LHS is selected from the group consisting of LHSa and LHSb And wherein, the asterisk (*) marks the point of attachment; These compounds exhibit antibacterial activity against Gram-negative and Gram-positive bacteria, especially S. aureus, E. coli, K. pneumoniae and A. baumannii. Pharmaceutical compositions containing these compounds, therapeutic uses thereof and methods for manufacturing the same are also provided.
Total Synthesis of Malacidin A by β-Hydroxyaspartic Acid Ligation-Mediated Cyclization and Absolute Structure Establishment
Brady, Sean F.,Chen, Sheng,Forelli, Nicholas,Li, Xuechen,Po, Kathy Hiu Laam,Shang, Zhuo,Sun, Zhenquan
supporting information, p. 19868 - 19872 (2020/09/02)
The development of novel antibiotics is critical to combating the growing emergence of drug-resistant pathogens. Malacidin A is a new member of the calcium-dependent antibiotic (CDAs) family with activity against antibiotic-resistant pathogens. Its mode of action is distinct from classical CDAs. However, the absolute structure of malacidin A has not been established. Herein, the total syntheses of malacidin A and its analogues are reported by a combination of Fmoc-based solid-phase peptide synthesis (SPPS) and β-hydroxyaspartic acid ligation-mediated peptide cyclization. The total synthesis enabled us to establish the absolute configuration of malacidin A, which is in agreement with those for natural malacidin A confirmed by advanced Marfey's analysis in our study.
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.
supporting information, 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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Paragraph 0144; 0145; 0146; 0147, (2015/09/22)
no abstract published
Hepatitis C Virus Inhibitors
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Paragraph 0318; 0319, (2015/11/02)
Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
An experimental and theoretical study on free ligand conformational preferences and enantioselectivity relationship for the asymmetric addition of diethylzinc to benzaldehyde
Wang, Min-Can,Liu, Zhi-kang,Li, Song,Ding, Xue,Li, Yuan,Tang, Ming-Sheng
experimental part, p. 486 - 493 (2010/06/20)
An experimental and theoretical study on free ligand conformational preferences and enantioselectivity relationship has been described for the asymmetric addition of diethylzinc to benzaldehyde. The results show that a correlation must exist between the ground-state ligand conformational populations and the observed ee values in this reaction. As the populations of the free ligand conformation (the desired conformation) in favor of the improvement of the reaction enantioselectivity increase, so does the reaction enantioselectivity. However, the desired conformation must not be the preferred one of the ground-state ligand. This conformation-enantioselectivity relationship is well explained based on a zinc amino-alkoxide (a true asymmetric catalyst). The final synthesis and assessment of the new chiral catalyst in the asymmetric addition of Et2Zn to benzaldehyde revealed that this necessary relationship guided our design of highly enantioselective ligands or rational improvement of existing ligands by means of knowledge of conformational analysis.
UREA DERIVATIVES AS ANTIBACTERIAL AGENTS
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Page/Page column 57-58, (2010/04/03)
This invention relates to compounds of the Formula (I):or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
ORGANIC COMPOUNDS FOR APPLICATIONS IN BACTERIAL INFECTIONS TREATMENT
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Page/Page column 58-59, (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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Page/Page column 234, (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.
CHIRAL FUSED [1,2]IMIDAZO[4,5-c] RING COMPOUNDS
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Page/Page column 159, (2008/06/13)
Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a -CH(-X1-R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
