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

CK Cusumano, JS Pinkner, Z Han, SE Greene… - Science translational …, 2011 - science.org
Chronic and recurrent urinary tract infections pose a serious medical problem because there
are few effective treatment options. Patients with chronic urinary tract infections are …

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

T Klein, D Abgottspon, M Wittwer… - Journal of medicinal …, 2010 - ACS Publications
Urinary tract infection (UTI) by uropathogenic Escherichia coli (UPEC) is one of the most
common infections, particularly affecting women. The interaction of FimH, a lectin located at …

FimH antagonists: bioisosteres to improve the in vitro and in vivo PK/PD profile

S Kleeb, L Pang, K Mayer, D Eris, A Sigl, RC Preston… - 2015 - ACS Publications
Urinary tract infections (UTIs), predominantly caused by uropathogenic Escherichia coli
(UPEC), belong to the most prevalent infectious diseases worldwide. The attachment of …

FimH Antagonists: Structure–Activity and Structure–Property Relationships for Biphenyl α‐D‐Mannopyranosides

L Pang, S Kleeb, K Lemme, S Rabbani… - …, 2012 - Wiley Online Library
Urinary tract infections (UTIs) are caused primarily by uropathogenic Escherichia coli
(UPEC), which encode filamentous surface‐adhesive organelles called type 1 pili. FimH is …

Rational design strategies for FimH antagonists: new drugs on the horizon for urinary tract infection and Crohn's disease

LK Mydock-McGrane, TJ Hannan… - Expert opinion on drug …, 2017 - Taylor & Francis
ABSTRACT Introduction: The bacterial adhesin FimH is a virulence factor and an attractive
therapeutic target for urinary tract infection (UTI) and Crohn's Disease (CD). Located on type …

Antivirulence isoquinolone mannosides: optimization of the biaryl aglycone for FimH lectin binding affinity and efficacy in the treatment of chronic UTI

C Jarvis, Z Han, V Kalas, R Klein, JS Pinkner… - …, 2016 - Wiley Online Library
Uropathogenic E. coli (UPEC) employ the mannose‐binding adhesin FimH to colonize the
bladder epithelium during urinary tract infection (UTI). Previously reported FimH antagonists …

Antiadhesion Therapy for Urinary Tract Infections A Balanced PK/PD Profile Proved To Be Key for Success

X Jiang, D Abgottspon, S Kleeb… - Journal of medicinal …, 2012 - ACS Publications
The initial step for the successful establishment of urinary tract infections (UTIs),
predominantly caused by uropathogenic Escherichia coli, is the adhesion of bacteria to …

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

O Schwardt, S Rabbani, M Hartmann… - Bioorganic & medicinal …, 2011 - Elsevier
Urinary tract infection (UTI) caused by uropathogenic Escherichia coli (UPEC) is one of the
most prevalent infectious diseases. Particularly affected are women, who have a 40–50 …

Combinatorial small-molecule therapy prevents uropathogenic Escherichia coli catheter-associated urinary tract infections in mice

PS Guiton, CK Cusumano, KA Kline… - Antimicrobial agents …, 2012 - Am Soc Microbiol
Catheter-associated urinary tract infections (CAUTIs) constitute the majority of nosocomial
urinary tract infections (UTIs) and pose significant clinical challenges. These infections are …

FimH and anti-adhesive therapeutics: a disarming strategy against uropathogens

M Sarshar, P Behzadi, C Ambrosi, C Zagaglia… - Antibiotics, 2020 - mdpi.com
Chaperone-usher fimbrial adhesins are powerful weapons against the uropathogens that
allow the establishment of urinary tract infections (UTIs). As the antibiotic therapeutic …