Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 705-86-2, Name is 6-Pentyltetrahydro-2H-pyran-2-one, molecular formula is C10H18O2, belongs to Triazoles compound, is a common compound. In a patnet, author is Tomasic, Tihomir, once mentioned the new application about 705-86-2, COA of Formula: C10H18O2.
Does targeting Arg98 of FimH lead to high affinity antagonists?
Bacterial resistance has become an important challenge in the treatment of urinary tract infections. The underlying resistance mechanisms can most likely be circumvented with an antiadhesive approach, antagonizing the lectin FimH located at the tip of flmbriae of uropathogenic E. coli. Here we report on a novel series of FimH antagonists based on the 1-(alpha-D-mannopyranosyl)-4-phenyl-1,2,3-triazole scaffold, designed to incorporate carboxylic acid or ester functions to interact with FimH Arg98. The most potent representative of the series, ester 11e, displayed a K-d value of 7.6 nM for the lectin domain of FimH with a general conclusion that all esters outperform carboxylates in terms of affinity. Surprisingly, all compounds from this new series exhibited improved binding affinities also for the R98A mutant, indicating another possible interaction contributing to binding. Our study on 1-(alpha-D-mannopyranosyl)-4-phenyl-1,2,3-triazole-based FimH antagonists offers proof that targeting Arg98 side chain by a chemical common sense, i.e. by introduction of the acidic moiety to form ionic bond with Arg98 is most likely unsuitable approach to boost FimH antagonists’ potency. (C) 2020 Elsevier Masson SAS. All rights reserved.
We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 705-86-2. The above is the message from the blog manager. COA of Formula: C10H18O2.