Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education

Chengdu, China

Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education

Chengdu, China
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Cheng C.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Liu Y.,H. Lee Moffitt Cancer Center and Research Institute | Song H.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Pan L.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | And 5 more authors.
Marine Drugs | Year: 2013

Methicillin-resistant Staphylococcus aureus (MRSA) continues to be a major problem, causing severe and intractable infections worldwide. MRSA is resistant to all beta-lactam antibiotics, and alternative treatments are limited. A very limited number of new antibiotics have been discovered over the last half-century, novel agents for the treatment of MRSA infections are urgently needed. Marinopyrrole A was reported to show antibiotic activity against MRSA in 2008. After we reported the first total synthesis of (±)-marinopyrrole A, we designed and synthesized a series of marinopyrrole derivatives. Our structure activity relationship (SAR) studies of these novel derivatives against a panel of Gram-positive pathogens in antibacterial assays have revealed that a para-trifluoromethyl analog (33) of marinopyrrole A is ≥63-, 8-, and 4-fold more potent than vancomycin against methicillin-resistant Staphylococcus epidermidis (MRSE), methicillin-susceptible Staphylococcus aureus (MSSA) and MRSA, respectively. The results provide valuable information in the search for new-generation antibiotics. © 2013 by the authors.


Huang J.-S.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Huang J.-S.,University of Sichuan | Huang W.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Huang W.,University of Sichuan | And 8 more authors.
Angewandte Chemie - International Edition | Year: 2015

An efficient methodology for the synthesis of α-Kdo glycosidic bonds has been developed with 5,7-O-di-tert-butylsilylene (DTBS) protected Kdo ethyl thioglycosides as glycosyl donors. The approach permits a wide scope of acceptors to be used, thus affording biologically significant Kdo glycosides in good to excellent chemical yields with complete α-selectivity. The synthetic utility of an orthogonally protected Kdo donor has been demonstrated by concise preparation of two α-Kdo-containing oligosaccharides. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Liu Q.-W.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Bin H.-C.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Yang J.-S.,Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education | Yang J.-S.,University of Sichuan
Organic Letters | Year: 2013

A new β-stereoselective d- and l-arabinofuranosylation method has been developed employing 5-O-(2-quinolinecarbonyl) substituted arabinosyl ethyl thioglycosides as glycosyl donors. The approach allows a wide range of acceptor substrates to be used; the β-selectivity is good-to-excellent. Stereoselective synthesis of a mannose-capped octasaccharide portion from a mycobacterial cell wall polysaccharide was then carried out to demonstrate the utility of this methodology. © 2013 American Chemical Society.

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