- Macrocyclic lactone compound, preparation method thereof, and intermediate application
-
The invention discloses macrolide compounds with the general structure represented by formula I, a preparation method thereof, an application thereof and an intermediate thereof. The macrolide compounds have very strong activities on most test G bacteria, wherein the activities of two types of compounds to partial gram-positive bacteria are higher than the activities of Azithromycin to the partial gram-positive bacteria.
- -
-
Paragraph 0074; 0075
(2016/10/07)
-
- A red ycin A derivatives, its preparation method, intermediate and application
-
The invention discloses an erythrocin A derivative represented by a general formula I. R1 and R2 are independent H, C1-C6 alkyl, replaced or not replaced C6-C10 aryl, or replaced or not replaced C4-C8 miscellaneous aryl; or the R1 and R2 are connected to form (CH2)n, wherein n is from 2 to 7; the substituent group of the aryl or the miscellaneous aryl is one type or a plurality of types of halogen, nitro, R3R4N-, C1-C6 alkoxy, C1-C6 alkyl and C6-C10 aryl, the heteroatom of the miscellaneous aryl is S, O or N, the number of the heteroatom in the miscellaneous aryl is from one to three, and R3 and R4 are the independent C1-C6 alkyl. The invention further discloses a preparation method of the compound I, an intermediate and an application. The compound has high antimicrobial activity particularly to a G+ bacterium.
- -
-
Paragraph 0101; 0102
(2016/10/10)
-
- Synthesis of di- and tri-saccharide fragments of Salmonella typhi Vi capsular polysaccharide and their zwitterionic analogues
-
Zwitterionic polysaccharides (ZPS) behave like traditional T cell-dependent antigens, suggesting the design of new classes of vaccines alternative to currently used glycoconjugates and based on the artificial introduction of a zwitterionic charge motif onto the carbohydrate structure of pathogen antigens. Here we report the new synthesis and antigenic evaluation of di-/tri-saccharide fragments of Salmonella typhi Vi polysaccharide, as well as of their corresponding zwitterionic analogues. Our strategy is based on versatile intermediates enabling chain elongation either by iterative single monomer attachment or by faster and more flexible approach using disaccharide donors. The effect of structural modifications of the synthetic compounds on antigenic properties was evaluated by competitive ELISA. All the oligosaccharides were recognized by specific anti-Vi polyclonal antibodies in a concentration-dependent manner, and the introduction of a zwitterionic motif into the synthetic molecules did not prevent the binding.
- Fusari, Matteo,Fallarini, Silvia,Lombardi, Grazia,Lay, Luigi
-
supporting information
p. 7439 - 7447
(2015/11/27)
-
- TYROSINE KINASE INHIBITORS
-
The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
- -
-
Page/Page column 146-147
(2011/08/03)
-