Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationship
about
The Prodrug Approach: A Successful Tool for Improving Drug SolubilityTricyclic GyrB/ParE (TriBE) inhibitors: a new class of broad-spectrum dual-targeting antibacterial agentsModeling & Informatics at Vertex Pharmaceuticals Incorporated: our philosophy for sustained impact.Challenges of antibacterial discoveryA high-throughput fluorescence polarization assay for inhibitors of gyrase BDual targeting antibacterial peptide inhibitor of early lipid A biosynthesis.Selective syntheses of no-carrier-added 2- and 3-[18F]fluorohalopyridines through the radiofluorination of halopyridinyl(4'-methoxyphenyl)iodonium tosylates.Inactivation of multiple bacterial histidine kinases by targeting the ATP-binding domain.A novel inhibitor of gyrase B is a potent drug candidate for treatment of tuberculosis and nontuberculosis mycobacterial infections.Evaluation of gyrase B as a drug target in Mycobacterium tuberculosis.Avalanche for shape and feature-based virtual screening with 3D alignment.Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.Clostridium difficile drug pipeline: challenges in discovery and development of new agentsDiscovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.Discovery of Novel Mycobacterial DNA Gyrase B Inhibitors: In Silico and In Vitro Biological Evaluation.On the Mechanism of Berberine-INF55 (5-Nitro-2-phenylindole) Hybrid AntibacterialsModification of agonist binding moiety in hybrid derivative 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-1-ol/-2-amino versions: impact on functional activity and selectivity for dopamine D2/D3 receptorsCalculating the sensitivity and robustness of binding free energy calculations to force field parameters.A simple, efficient synthesis of 2-aryl benzimidazoles using silica supported periodic Acid catalyst and evaluation of anticancer activity.Biological evaluation of benzothiazole ethyl urea inhibitors of bacterial type II topoisomerases.Bacterial DNA replication enzymes as targets for antibacterial drug discovery.Multitarget ligands in antibacterial research: progress and opportunities.Designing of inhibitors against drug tolerant Mycobacterium tuberculosis (H37Rv).Iterative refinement of a binding pocket model: active computational steering of lead optimization.Biophysical Studies of Bacterial Topoisomerases Substantiate Their Binding Modes to an InhibitorIdentification of 5,6-dihydroimidazo[2,1-b]thiazoles as a new class of antimicrobial agents.Synthesis of Berberine-Efflux Pump Inhibitor Hybrid Antibacterials.Berberine-INF55 (5-nitro-2-phenylindole) hybrid antimicrobials: effects of varying the relative orientation of the berberine and INF55 components.Synthesis and in-vitro antimycobacterial activity of fluoroquinolone derivatives containing a coumarin moiety.A rapid and efficient route to benzazole heterocycles.Evaluation of WO2012177707 and WO2012097269: Vertex's phosphate prodrugs of gyrase and topoisomerase antibacterial agents.Design, synthesis, and biological evaluation of 1-ethyl-3-(thiazol-2-yl)urea derivatives as Escherichia coli DNA gyrase inhibitors.Synthesis and Evaluation of N-Phenylpyrrolamides as DNA Gyrase B Inhibitors.
P2860
Q26771271-C163010E-7F58-4F44-8D8B-6E1DD5803762Q28538023-94157931-4305-4C28-AC71-E3A6F114A3FAQ30395805-7350CA15-D1DA-4DE3-9731-32009A96699DQ33793074-9F8EC1AC-8FF3-47A9-BCDF-08EA42C855E4Q33796345-D26227C2-9EBD-424E-92E1-6F14AFB3D542Q34244177-24B0CAB9-6893-45D0-AA58-670410A89AFFQ34284995-8299A4BA-C987-453E-9D3A-D3DC4F00D61AQ34992446-A34A5BB1-B2B7-401B-B36E-99EA89CFBB32Q35076966-9625DEBF-536E-4A06-A92E-9C4FB050A9D9Q35662004-ACA66C76-D3DE-4254-ABB2-92A6BF6A24C7Q35803775-C33D7643-1C2E-46A0-9CDB-DADF8869878DQ35815665-8C80854D-77B7-4CFC-99A6-2303774577E8Q35844527-6612C913-6751-45DB-B03B-C0D2A31C6091Q35846436-F2ABFA67-496A-4C08-8D7D-E78C3F48549CQ35994500-325ED616-0231-4092-BFFC-20218998685EQ36093500-DE487C6A-3965-48CC-BC00-98887059F78FQ36485393-71358E1C-C961-4166-8C32-80E97BBA671AQ37140503-A2C1CFE0-DCFC-4A70-BD95-14A4F1E5C74BQ37149321-0FA836D8-4F85-4A3A-A8C3-54B61A9E138CQ37156576-8D14C591-8882-452C-95BB-6FF7FCB34610Q37335706-CC248363-D778-43FA-A1A3-DFDDC193F1CDQ37998090-21802D92-A901-4E0C-A2A9-F188745EBCF2Q38068475-A2BDCC1F-48CC-4E86-812C-31188E52F70DQ40235240-7729BA8F-F0F4-4321-B0C0-10E21AB015C0Q40255869-AC266D49-29EA-445F-9A23-F84743764FA0Q40356984-D3C545F2-6576-4C6E-A768-382C34C548FBQ40529090-B641CD8A-1F91-496F-9BBB-158F8B87E0D7Q42030710-1FF1F2F7-4AB7-485F-97EB-C694213594E1Q42577087-528BD484-51B9-4D08-BBD2-6E031B90D387Q42726128-01CC7EE7-9488-461D-B9B7-10BB86057A0AQ42844160-1E1FE59F-01CC-4023-BC3B-434B2DC121F6Q43473553-11C7F411-D7E9-4BB8-B775-76DB07B5DDF9Q48120268-7C0A7AB5-0E05-4A69-B005-1A6AF2D3D3C7Q48175813-CD3F0E77-DCC7-4D81-BDEF-ED11E4A6B2D4
P2860
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationship
description
2008 nî lūn-bûn
@nan
2008年の論文
@ja
2008年学术文章
@wuu
2008年学术文章
@zh
2008年学术文章
@zh-cn
2008年学术文章
@zh-hans
2008年学术文章
@zh-my
2008年学术文章
@zh-sg
2008年學術文章
@yue
2008年學術文章
@zh-hant
name
Novel dual-targeting benzimida ...... tructure-activity relationship
@en
Novel dual-targeting benzimida ...... tructure-activity relationship
@nl
type
label
Novel dual-targeting benzimida ...... tructure-activity relationship
@en
Novel dual-targeting benzimida ...... tructure-activity relationship
@nl
prefLabel
Novel dual-targeting benzimida ...... tructure-activity relationship
@en
Novel dual-targeting benzimida ...... tructure-activity relationship
@nl
P2093
P356
P1476
Novel dual-targeting benzimida ...... tructure-activity relationship
@en
P2093
Anne-Laure Grillot
Arnaud LeTiran
Christian H Gross
David D Deininger
David P Nicolau
Dean Shannon
Dean Stamos
Emanuele Perola
Hong Zhang
Jonathan D Parsons
P304
P356
10.1021/JM800318D
P407
P577
2008-08-09T00:00:00Z