55592-81-9Relevant academic research and scientific papers
DEUTERATED TETRAPEPTIDES THAT TARGET MITOCHONDRIA
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Page/Page column 38, (2019/06/05)
Disclosed are deuterated analogs of SBT-20 and elamipretide (MTP-131). The compounds are useful for the treatment and prevention of ischemia-reperfusion injury (e.g., cardiac ischemia-reperfusion injury) or myocardial infarction.
CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE
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Paragraph 0131-0135, (2017/10/24)
The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as showed by formula I. In detail, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease
Lohou, Elodie,Sasaki, N. André,Boullier, Agnès,Sonnet, Pascal
, p. 702 - 722 (2016/07/26)
An important part of pathogenesis of Alzheimer's disease (AD) is attributed to the contribution of AGE (Advanced Glycation Endproducts) and ALE (Advanced Lipid peroxidation Endproducts). In order to attenuate the progression of AD, we designed a new type of molecules that consist of two trapping parts for reactive carbonyl species (RCS) and reactive oxygen species (ROS), precursors of AGE and ALE, respectively. These molecules also chelate transition metals, the promoters of ROS formation. In this paper, synthesis of the new AGE/ALE inhibitors and evaluation of their physicochemical and biological properties (carbonyl trapping capacity, antioxidant activity, Cu2+-chelating capacity, cytotoxicity and protective effect against in?vitro MGO-induced apoptosis in the model AD cell-line PC12) are described. It is found that compounds 40b and 51e possess promising therapeutic potentials for treating AD.
One-pot synthesis of orthogonally protected dipeptide selenazoles employing Nα-amino selenocarboxamides and α-bromomethyl ketones
Madhu, Chilakapati,Panguluri, Nageswara Rao,Narendra,Panduranga,Sureshbabu, Vommina V.
supporting information, p. 6831 - 6835 (2015/01/09)
A simple and efficient protocol for the synthesis of selenazole containing dipeptidomimetics using Nα-amino selenocarboxamides and α-bromomethyl ketones is described. All the compounds made were isolated in good yields and fully characterized.
Solution-phase synthesis of a muramyl dipeptide analogue MDA
Zhao, Nan,Ma, Yao,Liu, Gang
scheme or table, p. 1443 - 1446 (2012/06/04)
The solution-phase synthesis of a muramyl dipeptide (MDP) analogue of Nα-[4-chlorocinnamoyl-l-alanyl-d-isoglutaminyl]-l-lysine (MDA, 2) is reported that possesses the features of easy feasibility, safety and low cost in large scale of synthesis.
A simple synthesis of imide-dipeptides
Ke, Damei,Zhan, Chuanlang,Li, Xiao,Li, Alexander D. Q.,Yao, Jiannian
experimental part, p. 1506 - 1510 (2009/12/24)
We report a simple approach to synthesize a new class of imide-dipeptides. This approach is mild, and the starting materials are the easily accessible amino acid derivatives. The imide-dipeptides were synthesized from the coupling of an amide and a 4-nitrophenyl activating ester of an amino acid. The acidic proton of the first amide was removed by 1 equivalent of n-butyl lithium to afford the corresponding amide anion which then reacted with the activating ester to give the desired imide derivatives. Georg Thieme Verlag Stuttgart.
C-Terminally PEGylated hGH-derivatives
Peschke, Bernd,Zundel, Magali,Bak, Sonja,Clausen, Trine R.,Blume, Niels,Pedersen, Anja,Zaragoza, Florencio,Madsen, Kjeld
, p. 4382 - 4395 (2008/03/13)
A two-step strategy was used for the preparation of C-terminally PEGylated hGH-derivatives. In a first step a CPY-catalyzed transpeptidation was performed on hGH-Leu-Ala, introducing reaction handles, which were used in the second step for the ligation of
COUPLING OF POLYPEPTIDES AT THE C-TERMINUS
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Page/Page column 38, (2008/06/13)
The present invention relates to novel polypeptides, methods for their synthesis, pharmaceutical compositions comprising the novel polypeptides as well as their use in medicaments for therapeutic applications.
C-TERMINALLY PEGYLATED GROWTH HORMONES
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Page/Page column 93, (2008/06/13)
7150.204-WO 141 ABSTRACT Conjugated growth hormones of the structure O NH2 GH Leu N H G PEG [I] are provided together with methods for manufacturing said conjugates. The conjugates are 5 useful in therapy.
Synthesis of peptidoglycan units with UDP at the anomeric position
Lioux, Thierry,Busson, Roger,Rozenski, Jef,Nguyen-Disteche, Martine,Frere, Jean-Marie,Herdewijn, Piet
, p. 1615 - 1641 (2007/10/03)
A series of UDP-disaccharide peptide compounds were synthesized as synthetic substrate analogues or potential inhibitors of glycosyl transferase. Fluorescent compounds have been prepared with the aim of developing a screening method for selecting transglycosylase inhibitors.
