共查询到20条相似文献,搜索用时 15 毫秒
1.
Vara Prasad JV Boyer FE Chupak L Dermyer M Ding Q Gavardinas K Hagen SE Huband MD Jiao W Kaneko T Maiti SN Melnick M Romero K Patterson M Wu X 《Bioorganic & medicinal chemistry letters》2006,16(20):5392-5397
We describe a novel class of benzocycloheptanone derived oxazolidinone antibacterial agents. The synthesis and antibacterial activities with structure variation is discussed. 相似文献
2.
Ji-Young Kim Frederick E. Boyer Allison L. Choy Michael D. Huband Paul J. Pagano J.V.N. Vara Prasad 《Bioorganic & medicinal chemistry letters》2009,19(2):550-553
A novel series of oxazolidinones were synthesized in which the morpholine C-ring of linezolid was replaced with homomorpholine. In addition to investigating the effect of a homomorpholine C-ring on antibacterial activity, the effect of des-, mono-, di-, and tri-fluoro substitution on the phenyl B-ring was investigated as well. Various C-5 functional groups were also examined, including acetamides and triazoles and carboxamides. 相似文献
3.
The structural similarity between beta-lactam antibiotics, such as penicillin, and isoxazolidine-3,5-dicarboxylic acids led to the hypothesis that isoxazolidine-3,5-dicarboxylic acids could be effective analogs of beta-lactam antibiotics. The syntheses of relevant isoxazolidine-3,5-dicarboxylic acids from acylnitroso Diels-Alder adducts and subsequent biological testing have shown that these first examples are inhibitors of Escherichia coli X580. 相似文献
4.
The oxazolidinones are a promising new class of synthetic antibacterial agents. Here, we review recent efforts directed at the discovery of new antibacterial compounds of this class. New structures and structure-activity relationships (SAR) are discussed in the context of earlier work in the field. Key issues of potency, spectrum, selectivity, in vivo efficacy, and pharmacokinetic profile of the new analogs are addressed. 相似文献
5.
6.
Lee JS Cho YS Chang MH Koh HY Chung BY Pae AN 《Bioorganic & medicinal chemistry letters》2003,13(22):4117-4120
A series of isoxazolyl tetrahydropyridinyl oxazolidinones with various substituents at the 3-position of the isoxazole ring have been synthesized and their in vitro antibacterial activities (MIC) were evaluated against several Gram-positive strains including the resistant strains of Staphyloccus and Enterococcus, such as MRSA and VRE. One of the most potent compounds synthesized, 4f, showed comparable or better activity against selected bacterial strains than those of linezolid and vancomycin. 相似文献
7.
Asher M. Siddiqui Jitendra A. Sattigeri Kalim Javed Syed Shafi M. Shamim Smita Singhal Zubbair M. Malik 《Bioorganic & medicinal chemistry letters》2018,28(7):1198-1206
Gram-positive bacteria are among the most common human pathogens associated with clinical infections which range from mild skin infections to sepsis. Resistance towards existing class of drugs by Gram-positive bacteria including methicillin resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE) and vancomycin resistant enterococci (VRE) is a growing concern. There is an urgent need to discover new antibiotics which are active against resistant strains of Gram positive bacteria. We report herein a novel class of spiropyrimidinetrione oxazolidinone derivatives as novel antibacterial agents. Key step towards the synthesis of title compounds involved the use of tert-amino reaction with [1,5]-hydride shift leading to the new CC bond formation. Compound 30n has demonstrated potent antibacterial activity against a panel of Gram-positive microbial strains including MRSA, MRSE, and LNZ and vancomycin resistant strains of E. faecalis. Further, molecular docking studies suggest that 30n has binding mode similar to that of LNZ in 50S RNA ribosome. 相似文献
8.
Ebner DC Culhane JC Winkelman TN Haustein MD Ditty JL Ippoliti JT 《Bioorganic & medicinal chemistry》2008,16(5):2651-2656
The oxazolidinone class of antimicrobials represents a promising advance in the fight against resistant Gram-positive bacterial infections. Four novel oxazolidinone antimicrobial compounds, each containing a benzodioxin ring system, have been prepared. The general synthesis of each compound begins with the construction of a benzodioxin ring system containing a nitro substituent that ultimately becomes the nitrogen of the oxazolidinone ring. Three of the compounds utilize high yielding 'click chemistry' in their final step. The antimicrobial activities of the new oxazolidinones have been measured and the MIC against Staphylococcus aureus for one of the antimicrobials was determined to be 2-3 microg/mL, which is comparable to the well-known oxazolidinone, linezolid. 相似文献
9.
Michael S. Visser Kevin D. Freeman-Cook Steven J. Brickner Katherine E. Brighty Phuong T. Le Sarah K. Wade Rhonda Monahan Gary J. Martinelli Kyle T. Blair Dianna E. Moore 《Bioorganic & medicinal chemistry letters》2010,20(22):6730-6734
Novel hygromycin A derivatives bearing a variety of functionalized aminocyclitol moieties have been synthesized in an effort to increase the antibacterial activity and drug-like properties of this class of agents. A systematic study of the effect of alkylation and removal of the hydroxyls of the aminocyclitol directed us to a series of alkylated aminocyclitol derivatives with improved Gram-positive activity. 相似文献
10.
《Bioorganic & medicinal chemistry letters》2019,29(23):126746
In this article, a series of novel oxazolidinone derivatives containing a piperidinyl moiety was designed and synthesized. Their antibacterial activities were measured against S. aureus, MRSA, MSSA, LREF and VRE by MIC assay. Most of them exhibited potent activity against Gram-positive pathogens comparable to linezolid. Among them, compound 9h exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9h, which showed remarkable antibacterial activity against S. aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.25–1 μg/mL, was an interesting candidate for further investigation. 相似文献
11.
Bin Guo Houxing Fan Qisheng Xin Wenjing Chu Hui Wang Yushe Yang 《Bioorganic & medicinal chemistry letters》2013,23(13):3697-3699
A number of benzoxazinyl-oxazolidinones bearing 3-trizolylmethyl or 3-carboxamide side chain were designed and synthesized with the aim to develop antibacterial agents with improved properties. In vitro antibacterial activities of these novel compounds were evaluated against a panel of resistant and susceptible Gram-positive bacteria. Most analogues bearing 3-trizolylmethyl showed good to moderate antibacterial activities. Compound 12a exhibited a fourfold increase in activity compared with linezolid against all the tested strains, which was identified to be a promising antibacterial agent for further evaluation. 相似文献
12.
Synthesis and biological evaluations of novel benzimidazoles as potential antibacterial agents 总被引:1,自引:0,他引:1
A series of novel benzimidazole derivatives were synthesized via parallel solution-phase chemistry. Many of these compounds were found to inhibit the growth of Staphylococcus aureus and Escherichia coli. Several analogues exhibited low micromolar minimal inhibitory concentrations (MIC) against both Gram-positive and Gram-negative bacteria of clinical relevance and could serve as leads for further optimizations for antibacterial research. 相似文献
13.
Khera MK Cliffe IA Mathur T Prakash O 《Bioorganic & medicinal chemistry letters》2011,21(10):2887-2889
The synthesis and antibacterial activity of 3-(4-([1,2,4]triazolo[4,3-a]pyrimidin-3-yl)phenyl)oxazolidin-2-ones is reported. Thiocarbonyl derivatives were found to be potent inhibitors of Gram-positive pathogens and compound 4l was two to fourfold more potent than Linezolid. 相似文献
14.
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents 总被引:2,自引:0,他引:2
Kim HY Lee JS Cha JH Pae AN Cho YS Chang MH Koh HY 《Bioorganic & medicinal chemistry letters》2003,13(13):2227-2230
We have prepared and evaluated the antibacterial activities of a series of substituted methylenepiperidinyl and methylenepyrrolidinyl oxazolidinones against several gram-positive strains including the resistant strains of Staphyloccus and Enterococcus, such as MRSA, CRSA, MSSA and VRE. Some of them showed comparable or superior in vitro activities (MIC) to vancomycin. 相似文献
15.
The bicyclic, C(2)-symmetric dicarboxylic acid obtained from the cycloaddition of fumaric acid to anthracene can readily be prepared in enantiomerically pure form on a large scale. Conversion of either enantiomer of the diacid into its corresponding bis-allylamide yields a selector unit, used as a building block in the synthesis of a chiral stationary phase (CSP). The terminal C-C double bonds in the selector unit were used in a hydrosilylation reaction involving a multifunctional hydrosilane to effect polymerization, crosslinking, and immobilization to the vinyl-silica used as support. A study of the enantiomer-discriminating abilities of the new CSP was made. Large separation factors were obtained for a series of benzodiazepinones, which were studied in further detail by the use of different retention modifiers. To some extent, rationalization of retention data has been achieved in terms of competition for hydrogen bonding. 相似文献
16.
The synthesis and antibacterial activity of 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinones is reported. Compound 3e with a 2,4-disubstituted thiophene ring was found to be a potent inhibitor of Gram-positive pathogens and was 4-16-fold more potent than Linezolid. 相似文献
17.
Tandon VK Yadav DB Singh RV Vaish M Chaturvedi AK Shukla PK 《Bioorganic & medicinal chemistry letters》2005,15(14):3463-3466
A series of 1,4-naphthoquinone derivatives were synthesized and evaluated for antibacterial and antiviral activities. The structure-activity relationships of these compounds were also studied. The results suggest that compounds 9-22 showed in vitro marked antibacterial activity. Compounds 4c and 7a showed inhibitory effect against RNA dependent RNA polymerase induced poliovirus type 2 infected HeLa cells. 相似文献
18.
Murphy ST Case HL Ellsworth E Hagen S Huband M Joannides T Limberakis C Marotti KR Ottolini AM Rauckhorst M Starr J Stier M Taylor C Zhu T Blaser A Denny WA Lu GL Smaill JB Rivault F 《Bioorganic & medicinal chemistry letters》2007,17(8):2150-2155
Several novel series of nitrile-containing fluoroquinolones with weakly basic amines are reported which have reduced potential for hERG (human ether-a-go-go gene) channel inhibition as measured by the dofetilide assay. The new fluoroquinolones are potent against both Gram-positive and fastidious Gram-negative strains, including Methicillin resistant Staphylococcus aureus and fluoroquinolone-resistant Streptococcus pneumoniae. Several analogs also showed low potential for human genotoxicity as measured by the clonogenicity test. Compounds 22 and 37 (designated PF-00951966 and PF-02298732, respectively), which had good in vitro activity and in vitro safety profiles, also showed good pharmacokinetic properties in rats. 相似文献
19.
Dixit PP Nair PS Patil VJ Jain S Arora SK Sinha N 《Bioorganic & medicinal chemistry letters》2005,15(12):3002-3005
A series of novel (un)substituted benzotriazolyl oxazolidinone derivatives has been synthesized and tested for in vitro antibacterial activities by MIC determination against a panel of susceptible and resistant Gram-positive and Gram-negative microorganisms, some of which are resistant to methicillin and vancomycin. Compounds 20, 21, 24, 29 and 30 from this series were found to be equipotent or more potent than linezolid in vitro. 相似文献
20.
A N Pae H Y Kim H J Joo B H Kim Y S Cho K I Choi J H Choi H Y Koh 《Bioorganic & medicinal chemistry letters》1999,9(18):2679-2684
Two series of oxazolidinone derivatives having substituted isoxazoles were synthesized and tested for antibacterial activities against several Gram-positive strains including the resistant strains of Staphylococcus and Enterococcus, such as MRSA, CRSA, MSSA and VRE. Some of them showed in vitro activities (MIC) comparable or superior to the reference compound vancomycin. 相似文献