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Your search keyword '"Han, Zhenfu"' showing total 6 results
Start Over Author "Han, Zhenfu" Journal journal of medicinal chemistry
6 results on '"Han, Zhenfu"'

1. Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology

Author

Damalanka, Vishnu C., primary, Han, Zhenfu, additional, Karmakar, Partha, additional, O’Donoghue, Anthony J., additional, La Greca, Florencia, additional, Kim, Tommy, additional, Pant, Shishir M., additional, Helander, Jonathan, additional, Klefström, Juha, additional, Craik, Charles S., additional, and Janetka, James W., additional

Published
2018
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3. Antivirulence C-Mannosides as Antibiotic-Sparing, Oral Therapeutics for Urinary Tract Infections

Author

Mydock-McGrane, Laurel, primary, Cusumano, Zachary, additional, Han, Zhenfu, additional, Binkley, Jana, additional, Kostakioti, Maria, additional, Hannan, Thomas, additional, Pinkner, Jerome S., additional, Klein, Roger, additional, Kalas, Vasilios, additional, Crowley, Jan, additional, Rath, Nigam P., additional, Hultgren, Scott J., additional, and Janetka, James W., additional

Published
2016
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6. Lead Optimization Studieson FimH Antagonists: Discovery of Potent and Orally Bioavailable Ortho-SubstitutedBiphenyl Mannosides.

Author

Han, Zhenfu, Pinkner, Jerome S., Ford, Bradley, Chorell, Erik, Crowley, Jan M., Cusumano, Corinne K., Campbell, Scott, Henderson, Jeffrey P., Hultgren, Scott J., and Janetka, James W.

Subjects
*BIOAVAILABILITY, *PHARMACOKINETICS, *MANNOSE, *BIPHENYL compounds, *BLOOD agglutination, *URINARY tract infections, *BIOFILMS, *LEAD
Abstract

Herein, we describe the X-ray structure-based designand optimization of biaryl mannoside FimH inhibitors. Diverse modificationsto the biaryl ring to improve druglike physical and pharmacokineticproperties of mannosides were assessed for FimH binding affinity basedon their effects on hemagglutination and biofilm formation along withdirect FimH binding assays. Substitution on the mannoside phenyl ringortho to the glycosidic bond results in large potency enhancementsseveral-fold higher than those of corresponding unsubstituted matchedpairs and can be rationalized from increased hydrophobic interactionswith the FimH hydrophobic ridge (Ile13) or “tyrosine gate”(Tyr137 and Tyr48) also lined by Ile52. The lead mannosides have increasedmetabolic stability and oral bioavailability as determined from invitro PAMPA predictive model of cellularpermeability and in vivo pharmacokinetic studies in mice, therebyrepresenting advanced preclinical candidates with promising potentialas novel therapeutics for the clinical treatment and prevention ofrecurring urinary tract infections. [ABSTRACT FROM AUTHOR]

Published
2012
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