Ontology highlight
ABSTRACT:
SUBMITTER: Maddirala AR
PROVIDER: S-EPMC6467771 | biostudies-literature | 2019 Jan
REPOSITORIES: biostudies-literature
Maddirala Amarendar Reddy AR Klein Roger R Pinkner Jerome S JS Kalas Vasilios V Hultgren Scott J SJ Janetka James W JW
Journal of medicinal chemistry 20190102 2
The F9/Yde/Fml pilus, tipped with the FmlH adhesin, has been shown to provide uropathogenic Escherichia coli (UPEC) a fitness advantage in urinary tract infections (UTIs). Here, we used X-ray structure guided design to optimize our previously described ortho-biphenyl Gal and GalNAc FmlH antagonists such as compound 1 by replacing the carboxylate with a sulfonamide as in 50. Other groups which can accept H-bonds were also tolerated. We pursued further modifications to the biphenyl aglycone result ...[more]