Tomasic, Tihomir; Rabbani, Said; Jakob, Roman P.; Reisner, Andreas; Jakopin, Ziga; Maier, Timm; Ernst, Beat; Anderluh, Marko published an article in 2021. The article was titled 《Does targeting Arg98 of FimH lead to high affinity antagonists?》, and you may find the article in European Journal of Medicinal Chemistry.Product Details of 14660-52-7 The information in the text is summarized as follows:
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 fimbriae of uropathogenic E. coli. Here we report on a novel series of FimH antagonists based on the 1-(α-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 I, displayed a Kd 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-(α-D-mannopyranosyl)-4-phenyl-1,2,3-triazole-based FimH antagonists offers proof that targeting Arg98 side chain by a “”chem. 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. After reading the article, we found that the author used Ethyl 5-bromovalerate(cas: 14660-52-7Product Details of 14660-52-7)
Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Product Details of 14660-52-7
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary