Bioorganic and Medicinal Chemistry Letters p. 2993 - 2997 (2018)
Update date:2022-08-02
Topics:
Sattigeri, Jitendra A.
Garg, Malvika
Bhateja, Pragya
Soni, Ajay
Rauf, Abdul Rehman Abdul
Gupta, Mahendrakumar
Deshmukh, Mahesh S.
Jain, Tarun
Alekar, Nidhi
Barman, Tarani Kanta
Jha, Paras
Chaira, Tridib
Bambal, Ramesh B.
Upadhyay, Dilip J.
Nishi, Takahide
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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Doi:10.1021/ja00497a028
(1979)Doi:10.1021/jo9000405
(2009)Doi:10.1021/jm100274c
(2010)Doi:10.1016/j.ejmech.2010.02.026
(2010)Doi:10.1002/pola.23976
(2010)Doi:10.1016/S0040-4020(01)86072-5
(1988)