排序方式: 共有35条查询结果,搜索用时 15 毫秒
1.
Pragnesh K. Panchal Pramod B. Pansuriya M. N. Patel 《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):453-458
Complexes of Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) with the Schiff bases salicylidene-o-aminothiophenol (H2L) and thiophene-o-carboxaldeneaniline (SB) have been synthesized and characterized by elemental analyses, magnetic measurements, thermogravimetric analyses as well as infrared spectra and reflectance spectra. The nature of the bonding has been discussed on the basis of IR spectral data. Magnetic susceptibility measurements and electronic spectral data suggest a six-coordinated octahedral structure for these complexes. The complexes of Mn(II), Co(II), Ni(II), Cu(II) are paramagnetic, while Zn(II) and Cd(II) are diamagnetic in nature. The complexes were tested for their antimicrobial activities against Salmonella typhi, Escherichia coli and Serratia marcescens using the “Disc Diffusion Method”. The results are compared with the standard drug (tetracycline) and show moderate activity. 相似文献
2.
Zahid H. Chohan M.A. Farooq Andrea Scozzafava Claudiu T. Supuran 《Journal of enzyme inhibition and medicinal chemistry》2013,28(1):1-7
Schiff bases derived from oxaldiamide/oxalylhydrazine and pyrrol-2-carbaldehyde, or salicylaldehyde respectively, as well as their Zn(II) complexes have been prepared and tested as antibacterial agents. These Schiff bases function as tetradentate ligands, forming octahedral Zn(II) complexes. The ketonic form for the diamide derived Schiff base and the enolic form of the hydrazide derived Schiff base were the preferred tautomers for coordination of the metal ions. The title compounds and their Zn(II) derivatives were evaluated for antibacterial activity against several bacterial strains which easily develop resistance to classical antibiotics, such as Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa. Some of them showed promising biological activity in inhibiting the growth of such organisms. 相似文献
3.
RNA is an extremely important target for the development of chemical probes of function or small molecule therapeutics. Aminoglycosides are the most well studied class of small molecules to target RNA. However, the RNA motifs outside of the bacterial rRNA A-site that are likely to be bound by these compounds in biological systems is largely unknown. If such information were known, it could allow for aminoglycosides to be exploited to target other RNAs and, in addition, could provide invaluable insights into potential bystander targets of these clinically used drugs. We utilized two-dimensional combinatorial screening (2DCS), a library-versus-library screening approach, to select the motifs displayed in a 3 × 3 nucleotide internal loop library and in a 6-nucleotide hairpin library that bind with high affinity and selectivity to six aminoglycoside derivatives. The selected RNA motifs were then analyzed using structure–activity relationships through sequencing (StARTS), a statistical approach that defines the privileged RNA motif space that binds a small molecule. StARTS allowed for the facile annotation of the selected RNA motif–aminoglycoside interactions in terms of affinity and selectivity. The interactions selected by 2DCS generally have nanomolar affinities, which is higher affinity than the binding of aminoglycosides to a mimic of their therapeutic target, the bacterial rRNA A-site. 相似文献
4.
Geng B Comita-Prevoir J Eyermann CJ Reck F Fisher S 《Bioorganic & medicinal chemistry letters》2011,21(18):5432-5435
An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity. 相似文献
5.
Miles TJ Barfoot C Brooks G Brown P Chen D Dabbs S Davies DT Downie DL Eyrisch S Giordano I Gwynn MN Hennessy A Hoover J Huang J Jones G Markwell R Rittenhouse S Xiang H Pearson N 《Bioorganic & medicinal chemistry letters》2011,21(24):7483-7488
As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via inhibition of bacterial topoisomerases II and IV. We have investigated various subunits in this series and report advanced studies on compound 7 which demonstrates good PK and in vivo efficacy properties. 相似文献
6.
Dieter Haebich Hein-Peter Kroll Hans-Georg Lerchen 《Bioorganic & medicinal chemistry letters》2009,19(22):6317-6318
Arginine–pyrimidine conjugates represent a novel class of compounds that exhibits therapeutic and prophylactic activity in lethal infections by Gram-positive and Gram-negative bacteria without showing antibacterial activity in vitro. 相似文献
7.
《Bioorganic & medicinal chemistry》2020,28(22):115710
In two previous studies, we identified compound 1 as a moderate GroEL/ES inhibitor with weak to moderate antibacterial activity against Gram-positive and Gram-negative bacteria including Bacillus subtilis, methicillin-resistant Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, and SM101 Escherichia coli (which has a compromised lipopolysaccharide biosynthetic pathway making bacteria more permeable to drugs). Extending from those studies, we developed two series of analogs with key substructures resembling those of known antibacterials, nitroxoline (hydroxyquinoline moiety) and nifuroxazide/nitrofurantoin (bis-cyclic-N-acylhydrazone scaffolds). Through biochemical and cell-based assays, we identified potent GroEL/ES inhibitors that selectively blocked E. faecium, S. aureus, and E. coli proliferation with low cytotoxicity to human colon and intestine cells in vitro. Initially, only the hydroxyquinoline-bearing analogs were found to be potent inhibitors in our GroEL/ES-mediated substrate refolding assays; however, subsequent testing in the presence of an E. coli nitroreductase (NfsB) in situ indicated that metabolites of the nitrofuran-bearing analogs were potent GroEL/ES inhibitor pro-drugs. Consequently, this study has identified a new target of nitrofuran-containing drugs, and is the first reported instance of such a unique class of GroEL/ES chaperonin inhibitors. The intriguing results presented herein provide impetus for expanded studies to validate inhibitor mechanisms and optimize this antibacterial class using the respective GroEL/ES chaperonin systems and nitroreductases from E. coli and the ESKAPE bacteria. 相似文献
8.
Mónica Uruburu Eloise Mastrangelo Martino Bolognesi Silvia Ferrara Giovanni Bertoni Mario Milani 《Journal of structural biology》2019,205(3):18-25
Pseudomonas aeruginosa is an opportunistic pathogen associated with severe diseases, such as cystic fibrosis. During an extensive search for novel essential genes, we identified tgpA (locus PA2873) in P. aeruginosa PAO1, as a gene playing a critical role in bacterial viability. TgpA, the translated protein, is an internal membrane protein with a periplasmic soluble domain, predicted to be endowed with a transglutaminase-like fold, hosting the Cys404, His448, and Asp464 triad. We report here that Cys404 mutation hampers the essential role of TgpA in granting P. aeruginosa viability. Moreover, we present the crystal structure of the TgpA periplasmic domain at 1.6?Å resolution as a first step towards structure–activity analysis of a new potential target for the discovery of antibacterial compounds. 相似文献
9.
目的:分析抗菌药物分级管理干预措施的实施及效果。方法:选择2011年5月至2013年5月间我院全院出院患者6622例的病案资料。其中实施分级管理制度之前的患者3238例,实施分级管理制度之后的患者3384例,分析分级管理前后医院抗菌药物使用情况。结果:实施分级管理制度后抗菌药物使用率,人均使用频次及人均抗菌药物费用均明显降低,与实施分级管理制度前比较差异具有统计学意义(P0.05)。实施分级管理制度后一线抗菌药物使用率显著提高,二线、三线抗菌药物使用率降低,与实施分级管理制度前比较差异具有统计学意义(P0.05)。实施分级管理后三联用药比例显著降低(P0.05),送检标本及检出阳性率较实施分级管理前无统计学意义(P0.05)。结论:实施抗菌药物分级管理可以有效的限制抗菌药物滥用情况,对于临床抗菌药物合理应用有积极意义。 相似文献
10.
Jean-Philippe Surivet Roland Lange Christian Hubschwerlen Wolfgang Keck Jean-Luc Specklin Daniel Ritz Daniel Bur Hans Locher Peter Seiler Daniel Stefan Strasser Lars Prade Christopher Kohl Christine Schmitt Gaëlle Chapoux Eser Ilhan Nadia Ekambaram Alcibiade Athanasiou Andreja Knezevic Daniela Sabato Alain Chambovey Pierre Wyss 《Bioorganic & medicinal chemistry letters》2012,22(21):6705-6711
A series of 2-amino-[1,8]-naphthyridine-3-carboxamides (ANCs) with potent inhibition of bacterial NAD+-dependent DNA ligases (LigAs) evolved from a 2,4-diaminopteridine derivative discovered by HTS. The design was guided by several highly resolved X-ray structures of our inhibitors in complex with either Streptococcus pneumoniae or Escherichia coli LigA. The structure–activity-relationship based on the ANC scaffold is discussed. The in-depth characterization of 2-amino-6-bromo-7-(trifluoromethyl)-[1,8]-naphthyridine-3-carboxamide, which displayed promising in vitro (MIC Staphylococcus aureus 1 mg/L) and in vivo anti-staphylococcal activity, is presented. 相似文献