Lead optimization studies on FimH antagonists: discovery of potent and orally bioavailable ortho-substituted biphenyl mannosides (Q36032748)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22449031%20AND%20SRC:MED&resulttype=core&format=json

27 January 2020

title

Lead optimization studies on FimH antagonists: discovery of potent and orally bioavailable ortho-substituted biphenyl mannosides (English)

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27 January 2020

3

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27 January 2020

James W. Janetka

10

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27 January 2020

9

Scott J Hultgren

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27 January 2020

author name string

Zhenfu Han

1

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27 January 2020

Jerome S Pinkner

2

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27 January 2020

Erik Chorell

4

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27 January 2020

Jan M Crowley

5

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27 January 2020

Corinne K Cusumano

6

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27 January 2020

Scott Campbell

7

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27 January 2020

Jeffrey P Henderson

8

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27 January 2020

language of work or name

English

0 references

publication date

13 April 2012

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Journal of Medicinal Chemistry

27 January 2020

published in

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27 January 2020

volume

55

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issue

8

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27 January 2020

page(s)

3945-3959

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Treatment and prevention of urinary tract infection with orally active FimH inhibitors

27 January 2020

cites work

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Protein thermal shifts to identify low molecular weight fragments

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Structure-Based Drug Design and Optimization of Mannoside Bacterial FimH Antagonists

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2 October 2017

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Positive selection identifies an in vivo role for FimH during urinary tract infection in addition to mannose binding.

2 October 2017

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2 October 2017

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2 October 2017

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2 October 2017

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Integrin-mediated host cell invasion by type 1-piliated uropathogenic Escherichia coli

2 October 2017

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Differential stability and trade-off effects of pathoadaptive mutations in the Escherichia coli FimH adhesin

2 October 2017

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Cyclic AMP-regulated exocytosis of Escherichia coli from infected bladder epithelial cells

2 October 2017

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Rationally designed small compounds inhibit pilus biogenesis in uropathogenic bacteria.

2 October 2017

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Mechanisms of uropathogenic Escherichia coli persistence and eradication from the urinary tract

2 October 2017

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The affinity of the FimH fimbrial adhesin is receptor-driven and quasi-independent of Escherichia coli pathotypes

2 October 2017

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Maturation of intracellular Escherichia coli communities requires SurA.

2 October 2017

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Structural and functional insights into the assembly of type 1 pili from Escherichia coli

2 October 2017

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Antagonists of the myelin-associated glycoprotein: a new class of tetrasaccharide mimics

2 October 2017

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Role of phase variation of type 1 fimbriae in a uropathogenic Escherichia coli cystitis isolate during urinary tract infection

2 October 2017

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Differential gene expression for investigation of Escherichia coli biofilm inhibition by plant extract ursolic acid

2 October 2017

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Differentiation and developmental pathways of uropathogenic Escherichia coli in urinary tract pathogenesis.

2 October 2017

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Effect of trimethoprim-sulfamethoxazole on recurrent bacteriuria and bacterial persistence in mice infected with uropathogenic Escherichia coli

2 October 2017

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Inhibition of adhesion of type 1 fimbriated Escherichia coli to highly mannosylated ligands

2 October 2017

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2 October 2017

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Structural basis of tropism of Escherichia coli to the bladder during urinary tract infection

2 October 2017

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2 October 2017

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Establishment of a persistent Escherichia coli reservoir during the acute phase of a bladder infection.

2 October 2017

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2 October 2017

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Prevention of mucosal Escherichia coli infection by FimH-adhesin-based systemic vaccination

2 October 2017

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Formation of asymmetric unit membrane during urothelial differentiation

2 October 2017

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Type 1 fimbrial expression enhances Escherichia coli virulence for the urinary tract

2 October 2017

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Uroplakins Ia and Ib, two major differentiation products of bladder epithelium, belong to a family of four transmembrane domain (4TM) proteins

2 October 2017

1 reference

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Aromatic alpha-glycosides of mannose are powerful inhibitors of the adherence of type 1 fimbriated Escherichia coli to yeast and intestinal epithelial cells

2 October 2017

1 reference

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Regulation of production of type 1 pili among urinary tract isolates of Escherichia coli

2 October 2017

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FimH antagonists for the oral treatment of urinary tract infections: from design and synthesis to in vitro and in vivo evaluation.

2 October 2017

1 reference

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Do Escherichia coli strains causing acute cystitis have a distinct virulence repertoire?

11 July 2018

1 reference

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Design, synthesis and biological evaluation of mannosyl triazoles as FimH antagonists

23 September 2018

1 reference

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Bi- and trivalent glycopeptide mannopyranosides as inhibitors of type 1 fimbriae-mediated bacterial adhesion: variation of valency, aglycon and scaffolding

23 September 2018

1 reference

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Synthetic multimeric heptyl mannosides as potent antiadhesives of uropathogenic Escherichia coli.

23 September 2018

1 reference

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Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

23 September 2018

1 reference

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Mannosylated G(0) dendrimers with nanomolar affinities to Escherichia coli FimH.

23 September 2018

1 reference

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Development of intracellular bacterial communities of uropathogenic Escherichia coli depends on type 1 pili.

23 September 2018

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Tri- and hexavalent mannoside clusters as potential inhibitors of type 1 fimbriated bacteria using pentaerythritol and triazole linkages.

23 September 2018

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Oligomannoside mimetics by glycosylation of 'octopus glycosides' and their investigation as inhibitors of type 1 fimbriae-mediated adhesion of Escherichia coli.

23 September 2018

1 reference

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Selective electrochemical glycosylation by reactivity tuning

23 September 2018

1 reference

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Intracellular bacterial biofilm-like pods in urinary tract infections.

23 September 2018

1 reference

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Palladium-catalyzed cross-coupling reaction of bis(pinacolato)diboron with 1-alkenyl halides or triflates: convenient synthesis of unsymmetrical 1,3-dienes via the borylation-coupling sequence

23 September 2018

1 reference

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Mast cell phagocytosis of FimH-expressing enterobacteria.

23 September 2018

1 reference

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Diazo transfer and click chemistry in the solid phase syntheses of lysine-based glycodendrimers as antagonists against Escherichia coli FimH

23 September 2018

1 reference

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Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes

21 October 2018

1 reference

12 December 2020

Inhibition of the type 1 fimbriae-mediated adhesion of Escherichia coli to erythrocytes by multiantennary alpha-mannosyl clusters: the effect of multivalency

1 reference

12 December 2020

Receptor binding studies disclose a novel class of high-affinity inhibitors of the Escherichia coli FimH adhesin

1 reference

12 December 2020

Evaluation of the carbohydrate recognition domain of the bacterial adhesin FimH: Design, synthesis and binding properties of mannoside ligands

1 reference

12 December 2020

PAMPA--critical factors for better predictions of absorption

1 reference

12 December 2020

Clustering of Escherichia coli type-1 fimbrial adhesins by using multimeric heptyl α-D-mannoside probes with a carbohydrate core

1 reference

12 December 2020

Induction and evasion of host defenses by type 1-piliated uropathogenic Escherichia coli

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12 December 2020

Identifiers

DOI

10.1021/JM300165M

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22449031%20AND%20SRC:MED&resulttype=core&format=json

27 January 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22449031%20AND%20SRC:MED&resulttype=core&format=json

27 January 2020

PubMed publication ID

22449031

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22449031%20AND%20SRC:MED&resulttype=core&format=json