[EN] ANTIBODY-DRUG CONJUGATES, THEIR PREPARATION AND THEIR THERAPEUTIC USE [FR] CONJUGUÉS DE MOLÉCULES BIOLOGIQUEMENT ACTIVES, RÉACTIFS ET MÉTHODES DE FABRICATION, ET UTILISATIONS THÉRAPEUTIQUES
Transkarbams (T) represent novel group of highly active, non-toxic transdermal permeation enhancers. This study was focused on the influence of small symmetrical terminal branching on their enhancing activity. Series of T with terminal methyl or ethyl branching was prepared and their permeation-enhancing activity was compared to that of their linear analogues. The results showed completely a different behaviour from similarly branched alcohols, supporting the key role of the ammonium-carbamate polar head in the enhancing activity of T. (C) 2008 Elsevier Ltd. All rights reserved.
Rothe et al., Journal fur praktische Chemie (Leipzig 1954), 1959, vol. <4> 8, p. 323,331
作者:Rothe et al.
DOI:——
日期:——
Interfacial polycondensation. VIII. Application to AB-type monomers
作者:J. R. Schaefgen、F. H. Koontz、R. F. Tietz
DOI:10.1002/pol.1959.1204013708
日期:1959.11
AbstractThe application of interfacial polycondensation to the preparation of several polyurethanes and polyamides from AB type monomers is described. The monomers are salts of aminoalkyl chloroformates and aminoacid chlorides, respectively. Differences in method and mechanism from the AA plus BB type interfacial polycondensation are discussed. Several new ring‐containing polymers were synthesized.
Properties and structure–activity studies of cyclic β-hairpin peptidomimetics based on the cationic antimicrobial peptide protegrin I
作者:John A. Robinson、Sasalu C. Shankaramma、Peter Jetter、Ursula Kienzl、Reto A. Schwendener、Jan W. Vrijbloed、Daniel Obrecht
DOI:10.1016/j.bmc.2005.01.009
日期:2005.3
The properties and structure-activity relationships (SAR) of a macrocyclic analogue of porcine protegrin I (PG-I) have been investigated. The lead compound, having the sequence cyclo-(-Leu-Arg-Leu-Lys-Lys-Arg-Arg-Trp-Lys-Tyr-Arg-Val-D-Pro-Pro-), shows antimicrobial activity against Gram-positive and -negative bacteria, but a much lower haemolytic activity and a much reduced ability to induce dye release from phosphatidylcholine/phosphatidylglycerol liposomes, when compared to PG-I. The enantiomeric form of the lead peptide shows comparable antimicrobial activity, a property shared with other cationic antimicrobial peptides acting on cell membranes. SAR studies involving the synthesis and biological profiling of over 100 single site substituted analogues, showed that the antimicrobial activity was tolerant to a large number of the substitutions tested. Some analogues showed slightly improved antimicrobial activities (2-4-fold lowering of MICs), whereas other substitutions caused large increases in haemolytic activity on human red blood cells. (c) 2005 Elsevier Ltd. All rights reserved.
Aminocarboxylic acids, amino alcohols, or the derivatives thereof, processes for production thereof, and pharmaceutical composition, containing at least one of these compounds