Novel dithiocarbamate carbapenems1 with anti-MRSA activity
摘要:
A new series of carbapenems, in which disubstituted-aminothiocarbonylthio moiety, directly attached to the C-2 position, were prepared and evaluated for their antibacterial potency. These analogs showed potent activity against high-level MRSA, Among them, 9e and 9i were found to exhibit good in vivo efficacy comparable to that of vancomycin, for mouse septicemia model with high-level MRSA. (C) 1997 Elsevier Science Ltd.
One-pot two-step dithiocarbamylation of styrenes: metal-free stereoselective synthesis of styrenyl dithiocarbamates
作者:Manas Mondal、Amit Saha
DOI:10.1039/d2ob00315e
日期:——
Styrenes have been functionalized to produce styrenyl dithiocarbamates by a one-pot two-step procedure without using any metal catalysts. Styrene was transformed into a bromo-derivative, which undergoes a domino nucleophilic substitution followed by elimination in the presence of a dithiocarbamate anion and triethylamine to produce trans-styrenyl dithiocarbamates exclusively. The reaction shows a wide
The present invention provides an inorganic-organic composite-treated zinc-plated steel sheet whose treated coatings do not contain any chromium and which is excellent in corrosion resistance after degreasing, coating adhesion and electrodeposition coating performance.
The inorganic-organic composite-treated zinc-plated steel sheet, which is obtained by forming a zinc phosphate coating, in a coating weight of 0.3 to 5 g/m
2
, on the zinc-plated steel sheet surface and forming thereon a post-treatment coating, in a coating weight of 0.01 to 1 g/m
2
, by using a post-treatment composition containing at least one compound (A) selected from the group consisting of thiocarbonyl group-containing compounds, sulfide group-containing compounds and guanidyl group-containing compounds, an organic resin (B), a crosslinking agent (C) and an inorganic corrosion inhibitor (D).
Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors
作者:Coco N. Kapanda、Giulio G. Muccioli、Geoffray Labar、Jacques H. Poupaert、Didier M. Lambert
DOI:10.1021/jm901323s
日期:2009.11.26
Monoglyceride lipase (MGL) inhibition may offer an approach in treating diseases in which higher 2-arachidonoyglycerol activity would be beneficial. We report here the synthesis and pharmacological evaluation of bis(dialkylaminethiocarbonyl)disulfide derivatives as irreversible MGL inhibitors. Inhibition occurs through interactions with MGL C208 and C242 residues, and these derivatives exhibit high inhibition selectivity over fatty acid amide hydrolase, another endocannabinoid-hydrolyzing enzyme.
Novel dithiocarbamate carbapenems with anti-MRSA activity
A new series of 1 beta-methyl carbapenems, in which a disubstituted-aminothiocarbonylthio moiety was attached to the C-2 position of the carbapenem nucleus, were prepared and evaluated for anti-MRSA activity. These derivatives showed good in vitro antibacterial activity against high-level MRSA, and the finding of good affinity for PBP-2' supported these results. Some of the compounds having favorable protein-binding affinity showed excellent in vivo anti-MRSA activity. (C) 1998 Elsevier Science Ltd. All rights reserved.