82409-04-9Relevant articles and documents
INJECTABLE SOLUTION AT PH 7 COMPRISING AT LEAST ONE BASAL INSULIN FOR WHICH THE PI IS FROM 5.8 TO 8.5 AND A CO-POLYAMINO ACID BEARING CARBOXYLATE CHARGES AND HYDROPHOBIC RADICALS
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Paragraph 0515, (2021/01/19)
A composition in the form of an injectable aqueous solution, whose pH consists from 6.0 to 8.0, including at least: a basal insulin whose isoelectric point includes from 5.8 to 8.5; a co-polyamino-acid bearing carboxylate charges and hydrophobic radicals Hy, the co-polyamino-acid being constituted of glutamic or aspartic units and said hydrophobic radicals Hy according to the following formula I:
Compositions comprising a biocidal polyamine
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Page/Page column 84; 85, (2014/10/16)
Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates t
B-Z transition of (dA-T)n duplexes induced by a spermine porphyrin-conjugate via an intermediate DNA conformation
Sasaki, Hideaki,Sasaki, Shigeki
, p. 9024 - 9026 (2013/09/24)
The spermine conjugate of the cationic porphyrin ligand (1) selectively induced the B-Z transition of the [(dA-T)n]2 sequence at low salt concentrations. The [(dG-C)n]2 sequence was not transformed into the Z-form. The B-Z transition was induced via an intermediate DNA conformation, which was formed by the external binding and formation of an assembly of 1 onto B-DNA.
Synthesis and binding properties of new selective ligands for the nucleobase opposite the AP site
Abe, Yukiko,Nakagawa, Osamu,Yamaguchi, Rie,Sasaki, Shigeki
experimental part, p. 3470 - 3479 (2012/08/08)
DNA is continuously damaged by endogenous and exogenous factors such as oxidative stress or DNA alkylating agents. These damaged nucleobases are removed by DNA N-glycosylase and form apurinic/apyrimidinic sites (AP sites) as intermediates in the base exci
Preparation and biological assessment of hydroxycinnamic acid amides of polyamines
Fixon-Owoo, Solomon,Levasseur, Frederic,Williams, Keith,Sabado, Thomas N.,Lowe, Mike,Klose, Markus,Mercier, A. Joffre,Fields, Paul,Atkinson, Jeffrey
, p. 315 - 334 (2007/10/03)
Many plants contain hydroxycinnamic acid conjugates of polyamines that are remarkably similar in general structure to the acylated polyamines found in spider and wasp toxins. In an effort to determine whether these compounds might play a role in the chemical defense of plants against arthropod pests we synthesized a variety of analogues of the coumaric (4-hydroxycinnamic) acid conjugates of di-, tri-, and tetraamines using common protection and acylation strategies. N1- and N8-coumaroyl spcrmidinc spermidine were tested in feeding trials with insect larvae including the European corn borer (Ostrinia nuhilalis), the tobacco budworm (Heliothis verescens) and the oblique banded leaf roller (Choristoneura rosaceana). Antifeedant assays with the rice weevil Sitophilus oryzae were also performed. Neither the naturally occurring coumaric acid conjugates of polyamines nor their analogues showed notable toxicity towards insects, despite precautions to maintain these easily oxidized materials in the wet diet. However, more direct bioassays of these compounds on glutamate dependent neuroreceptors including the deep abdominal extensor muscles of crayfish, or mammalian NMDA, 62, and AMPA receptors, clearly showed that these compounds were inhibitory. N1-Coumnaoryl spermine, a dodecyl and a cyclohexyl analogue were especially active at NMDA NR1/NR2B receptors. The latter had an IC50 of 300 μM in the crayfish. N1-Coumaroyl spermine had an IC50 in the crayfish preparation of 70-300 μM and against the mammalian NR1/ NR2B receptor of 38 nM. Structure-activity variations show similar trends of length and hydrophobicity as has been seen previously with analogues of spider toxins. We conclude from this work that while the coumaric acid polyamine conjugates are active when directly applied to neuroreceptors, they show no overt toxicity when ingested by insect larvae.
Synthesis of Carbamate Protected Spermidine Homologues Through α,ω-Alkanediamines
Arasujo, M. Joso S. M. P.,Ragnarsson, Ulf,Trigo, M. Joaquina S. A. Amaral,Almeida, M. Lurdes S.
, p. 2143 - 2161 (2007/10/03)
The total synthesis of three triamines selectively protected in the primary amino groups (1a-c) and two triamines protected in the secondary amino function and in one of the primary amino functions (2a and 2c), based on a simple and efficient procedure, is described.
Efficient syntheses of polyamine and polyamine amide voltage-sensitive calcium channel blockers: FTX-3.3 and sFTX-3.3
Moya, Eduardo,Blagbrough, Ian S.
, p. 179 - 182 (2007/10/03)
Efficient syntheses of FTX-3.3 and sFTX-3.3, voltage-sensitive calcium channel blockers are described. These modified polyamines were prepared from selectively protected polyamines and purified on a practical scale.
Total Synthesis of Polyamine Amide Spider Toxin Argiotoxin-636 by a Practical Reductive Alkylation Strategy
Blagbrough, Ian S.,Moya, Eduardo
, p. 9393 - 9396 (2007/10/02)
Reductive alkylation is a practical strategy for a total synthesis of spider toxin argiotoxin-636, a polyamine amide which is selective glutamate receptor antagonist and may have potential as a neuroprotective agent.Central to this synthesis are a Swern o
Rapid, Practical Syntheses of the Arginyl Polyamine sFTX-3.3: a Blocker of Voltage-Sensitive Calcium Channels
Moya, Eduardo,Blagbrough, S. Ian
, p. 2061 - 2062 (2007/10/02)
sFTX-3.3, a polyamine toxin analogue, has been synthesized from tri-CBZ-L-arginine.Rapid, practical procedures to prepare this calcium channel blocker are presented.
