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Updated: Feb 7, 2026

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
Published on: October 26, 2017
Synthesis and evaluation of thiomannosides, potent and orally active FimH inhibitors
Jitendra A Sattigeri1, Malvika Garg1, Pragya Bhateja1
1Daiichi Sankyo India Pharma Pvt Ltd., Village Sarhaul, Sector 18, Udyog Vihar Industrial Area, Gurugram 122015, Haryana, India.
Abstract:
FimH is a type I fimbrial lectin located at the tip of type-1 pili of Gram-negative uropathogenic Escherichia coli (UPEC) guiding its ability to adhere and infect urothelial cells. Accordingly, blocking FimH with small molecule inhibitor is considered as a promising new therapeutic alternative to treat urinary tract infections caused by UPEC. Herein, we report that compounds having the S-glycosidic bond (thiomannosides) had improved metabolic stability and plasma exposures when dosed orally. Especially compound 5h showed the potential to inhibit biofilm formation and also to disrupt the preformed biofilm. And compound 5h showed prophylactic effect in UTI model in mice.
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