Synthesis and Bioactivity Investigation of the Individual Components of Cyclic Lipopeptide Antibiotics
摘要:
In this paper, 26 natural polymyxin components and a new derivative S-2 were synthesized, and their differences in efficacy and toxicity have been investigated. Almost all of the synthesized components showed strong activity against both susceptible and resistant strains of E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii. The toxicities were obviously different between the components. Only some of the components were tested for toxicity in vivo. Compounds E-2, E-2-Val, A(2), M-2, D-2, and S-2 showed obviously lower renal cytotoxicity and acute toxicity than polymyxins B and E. The in vivo nephrotoxicity of E-2, M-2, and S-2 was similar to that of polymyxin E. Compound S-2, with four positive charges, was especially interesting as it possessed both increased efficacy and decreased toxicity. The SAR and toxicity studies indicated that further structural modification could concentrate on polymyxin S. The results also indicated that S-2 could be a new drug candidate.
A Practical One-Pot Synthesis of Enantiopure Unsymmetrical Salen Ligands
作者:Michael Holbach、Xiaolai Zheng、Caroline Burd、Christopher W. Jones、Marcus Weck
DOI:10.1021/jo052614y
日期:2006.3.31
A practical, one-pot synthesis of enantiopure unsymmetrical salen ligands is described, using a 1:1:1 molar ratio of a chiral diamine and two different salicylaldehydes. The new synthetic protocol can be readily performed in good yields (60−85%) on a multigram scale with good tolerance toward various functional groups.
The present disclosure provides a polymerizable compound of the formula (I)
where the R
1
, R
2
, R′
1
, R′
2
, X
1
to X
8
, Y
1
, Y
2
, M and L have any of values as defined in the specification. The disclosure also provides an oligomer, a homo-polymer, or a co-polymer of compound of the formula (I). The disclosure also provides methods for preparing the compound of the formula (I) and methods for preparing polymers of the compound of the formula (I), and to methods and intermediates useful for preparing them. The disclosure also provides methods for the use of the polymers of formula (I) as chiral catalysts in enantioselective preparative processes.
Electrophoretic Dispersion Liquid and Electrophoretic Display Device
申请人:Minami Masato
公开号:US20080136772A1
公开(公告)日:2008-06-12
An electrophoretic dispersion liquid for an electrophoretic display apparatus includes a plurality of electrophoretic particles each surface of which is modified by one of a basic group and an acidic group, a liquid for holding said electrophoretic particles to be dispersed therein; and a polydiene, having the other group, dissolved in said liquid.
The purpose of the present invention is to provide an agglutination enhancer which shows superior agglutination enhancing effect to those of conventional immunoagglutination enhancers, and the present invention relates to an agglutination enhancer for an immunoagglutination measurement method which comprises a polymer having a monomer unit shown by the following general formula [1]:
(Wherein R
1
represents a hydrogen atom or a methyl group; R
2
and R
3
independently represent a methyl group or an ethyl group, respectively; X represents —NH— or an oxygen atom; n represents an integer of 1 to 6; and m represents an integer of 1 to 3), and an immunoagglutination measurement method in which, in the coexistence of the above-described agglutination enhancer for immunoagglutination measurement method, an antibody against analyte or an antigen for the analyte is brought into contact with the analyte to cause an antigen-antibody reaction.
According to the present invention there is provided a process for producing an acid anhydride by reacting a carboxylic acid, preferably a carboxylic acid having a polymerizable group, with a sulfonyl halide compound in the presence of a tertiary amine or in the presence of a tertiary amine and an inorganic base, wherein the tertiary amine or the tertiary amine and the inorganic base are used in an amount of 0.9 to 1.2 equivalents relative to the acid generated from the sulfonyl halide compound.