Lamellar Ni/Al-SBA-15 fibers: preparation, characterization, and applications as highly efficient catalysts for amine and imine syntheses
作者:Ren Ren、Jiantai Ma
DOI:10.1039/c5ra14382a
日期:——
A novel lamellar Ni/Al-SBA-15 fiber catalyst was prepared and successfully utilized in one-pot syntheses of amines and imines.
一种新型的层状Ni/Al-SBA-15纤维催化剂已经制备成功,并成功地用于胺和亚胺的一锅法合成。
Developing highly active small molecule ice recrystallization inhibitors based upon C-linked antifreeze glycoprotein analogues
作者:John F. Trant、Robyn A. Biggs、Chantelle J. Capicciotti、Robert N. Ben
DOI:10.1039/c3ra43835j
日期:——
Ice recrystallization during cryopreservation results in a significant amount of cellular damage making compounds that exhibit ice recrystallization inhibition (IRI) activity desirable as a novel class of cryoprotectants. Herein, we report a systematic structure–function study on a previously identified IRI active C-linked antifreeze glycoprotein (C-AFGP) analogue (1). These studies indicate that while C-AFGPs containing three tripeptide repeats exhibit weak IRI activity 5.5 μM, a minimum number of four tripeptide repeats is required for potent IRI activity at this concentration. In addition, the galactosyl–ornithine building block 5 exhibited only moderate activity at 22 mM, but IRI activity was significantly increased upon addition of two glycine units to the C-terminal end of the amino acid bearing the C-linked galactopyranose residue. Finally, we report that conjugation of long alkyl chains (octyl, nonyl and decyl) to the C-linked galactosyl moiety of 1 can furnish IRI active small molecules. The “ideal” hydrocarbon chain length was 10 carbons for potent activity in this series of compounds. Longer hydrocarbon chain lengths dramatically decreased solubilities. The results of this study emphasize the importance of hydrophobic moieties for IRI activity and while consistent with previously reported small molecule carbohydrate-based and lysine-based ice recrystallization inhibitors, is the first example where a large IRI active glycoconjugate has been successfully truncated to small molecule IRI active components.
Synthesis and antibacterial activity of new 4″-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether
作者:Ling Zhang、Bo Jiao、Xiangrui Yang、Lin Liu、Shutao Ma
DOI:10.1038/ja.2010.166
日期:2011.3
A series of new 4â³-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether were synthesized and evaluated for their in vitro antibacterial activity. All the desired compounds demonstrated favorable activity (0.03âμgâmlâ1) against erythromycin-susceptible Streptococcus pneumoniae comparable to the references, exhibiting 133-fold higher activity than precursor 2 or 3. Similarly, all of the analogs exhibited improved activity against the erythromycin-resistant S. pneumoniae encoded by the erm gene and the erm and mef genes, showing 4â32-fold more effectiveness than erythromycin A.
A full account on rhodium‐catalyzed asymmetric, directed hydroboration of functionalized prochiral cyclopropenes affording enantiomerically enriched cyclopropylboronates is reported. The scope and limitations of two alternate directing groups, ester and carboxamide, are evaluated. It was found that hydroboration of esters appeared to be more sensitive to substitution in the aromatic ring of the substrates
[EN] 1,4 DIHYDROPYRIDINE DERIVATIVES AND THEIR USES<br/>[FR] DÉRIVÉS DE LA 1,4-DIHYDROPYRIDINE ET LEURS UTILISATIONS
申请人:UNIV LILLE II DROIT & SANTE
公开号:WO2010133973A1
公开(公告)日:2010-11-25
The present invention relates to 1,4-dihydropyridine derivatives of the formula (I) and their uses in the treatment and/or prevention of diseases and disorders directly or indirectly associated with the modification (increase or decrease) of the activity of the cannabinoid receptor 2 (CB2).