67321-05-5Relevant articles and documents
Dual-acting agents that possess free radical scavenging and antithrombotic activities: Design, synthesis, and evaluation of phenolic tetrahydro-β-carboline RGD peptide conjugates
Bi, Wei,Bi, Lanrong,Cai, Jianhui,Liu, Sanguang,Peng, Shiqi,Fischer, Nicholas O.,Tok, Jeffrey B.-H.,Wang, Guohua
, p. 4523 - 4527 (2007/10/03)
A new approach to construct a single dual-acting agent is described. Compounds 6a-c are potent free radical scavengers as demonstrated by the EC50 values in PC12 cell survival assay in term of NO, H2O2, and {radical dot}OH scavenging activity. The Ach-induced vaso-relaxation assay further confirms the potent NO scavenging activity of compounds 6a-c. In addition, 6a-c are efficacious in a rat arterial thrombosis, and are active in ADP- or PAF-induced in vitro platelet aggregation assay, suggesting that compounds 6a-c also possess anti-thrombotic activities. Since both free radical and thrombogenesis are important risk factors in myocardial ischemic/reperfusion injuries, these dual-acting agents having both free radical scavenging and antithrombolic activities may potentially be beneficial toward their treatment.
Solution-phase automated synthesis of tripeptide derivatives
Kuroda,Hattori,Kitada,Sugawara
, p. 1138 - 1146 (2007/10/03)
An improved general method for automated synthesis of tripeptides was developed, in which methanesulfonic acid (MSA) was used in place of trifluoroacetic acid (TFA), thus making it possible to avoid, 1) corrosion of the apparatus by strong acid vapor, 2) formation of emulsions, and 3) use of the restricted solvent, dichloromethane. As an application of the automated synthesis apparatus, 216 fragment tripeptide derivatives were synthesized systematically using the MSA method, in excellent yield and with increased efficiency.
Chemo-enzymatic synthesis of glycopolymers and sequential glycopeptides bearing lactosamine and sialyl Lewisx unit pendant chains
Sallas, Florence,Nishimura, Shin-Ichiro
, p. 2091 - 2103 (2007/10/03)
A variety of glycoconjugates bearing either N-acetyllactosamine or sialyl Lewisx units have been synthesised in a chemo-enzymatic way. This includes the synthesis of glycopolymer copolymerised with acrylamide and whose glucosamine unit was substituted with different kinds of side-chain. Glycopeptides with different spacer-arm glucosamine units have also been prepared and polymerised. The sugar chain was then elongated using glycosyl transferases to afford the novel sequential glycopeptides. In these cases, the polymeric sugar cluster effect led to enzymatic glycosylation with high efficiency. Nevertheless, some differences have been noticed depending on the reaction conditions used for each substrate.
Application of a unique automated synthesis system for solution-phase peptide synthesis
Sugawara,Kobayashi,Okamoto,Kitada,Fujino
, p. 1272 - 1280 (2007/10/02)
An automated synthesis system, which is suitable for repetitive syntheses using similar reaction procedures, was used to synthesize systematically a library of all possible dipeptides (25) and tripeptides (125) from 5 protected amino acids. The apparatus has also been applied to the automated synthesis of 10 fragment tripeptide derivatives that are constituents of the hormone PACAP-27. The measured molecular optical rotation values of the library of 125 tripeptides were found to correlate well with calculated values obtained by summation of the molecular optical rotation values for the constituent amino acids.
[Asn2 ]-thymosin α1 and analogs thereof
-
, (2008/06/13)
Thymosin α1, was chemically synthesized by the fragment condensation of the protected amino terminal tetradecapeptide with the protected carboxyl terminal tetradecapeptide. Similarly prepared was the analog [Asn2 ]-thymosin α1 utilizing the appropriately modified protected amino terminal tetradecapeptide. Both products are active as agents which affect regulation, differentiation and function of thymus dependent lymphocytes (T cells).
