111-45-5Relevant articles and documents
9-(2-Aryloxyethyl) derivatives of adenine - A new class of non-nucleosidic antiviral agents
Petrov,Ozerov,Novikov,Pannecouque,Balzarini,De Clercq
, p. 1218 - 1226 (2003)
New 9-(aryloxyalkyl) derivatives of adenine have been prepared by alkylation of adenine with tosylates, bromides, and α-chloro ethers containing terminal aromatic fragments in anhydrous DMF in the presence of potassium carbonate. The compounds of the 9-(2-phenoxyethyl)adenine series appear to be highly reactive against cytomegaloviruses of mankind in vitro, while derivatives of 9-(2-benzyloxyethyl)adenine demonstrate anti-HIV-1 activity. Compounds with shorter or longer chains, and also compounds which do not have aromatic fragments at the ends of the chains, do not possess antiviral activity.
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Bertrand,M.P. et al.
, p. 1365 - 1372 (1979)
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Salt- and pH-Triggered Helix-Coil Transition of Ionic Polypeptides under Physiology Conditions
Yuan, Jingsong,Zhang, Yi,Sun, Yue,Cai, Zhicheng,Yang, Lijiang,Lu, Hua
, p. 2089 - 2097 (2018)
Controlling the helix-coil transition of polypeptides under physiological conditions is an attractive way toward smart functional materials. Here, we report the synthesis of a series of tertiary amine-functionalized ethylene glycol (EGx)-linked polypeptide electrolytes with their secondary structures tunable under physiological conditions. The resultant polymers, denoted as P(EGxDMA-Glu) (x = 1, 2, and 3), show excellent aqueous solubility (>20 mg/mL) regardless of their charge states. Unlike poly-l-lysine that can form a helix only at pH above 10, P(EGxDMA-Glu) undergo a pH-dependent helix-coil switch with their transition points within the physiological range (pH ~5.3-6.5). Meanwhile, P(EGxDMA-Glu) exhibit an unusual salt-induced helical conformation presumably owing to the unique properties of EGx linkers. Together, the current work highlights the importance of fine-tuning the linker chemistry in achieving conformation-switchable polypeptides and represents a facile approach toward stimuli-responsive biopolymers for advanced biological applications.
Chain extender as well as preparation method and application thereof
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Paragraph 0038; 0041; 0043; 0046; 0048; 0051, (2022/01/20)
The invention relates to a chain extender. The chain extender is 3-(2-(2, 3-dihydroxy propyl) sulfo) ethyoxyl) propyl 3-(3-(tert-butyl)-4-hydroxy-5-methyl phenyl) propionate (GL), and the structural formula of the chain extender is shown in the specification. The prepared chain extender GL has an excellent toughening effect; the elongation at break of a polyurethane elastomer prepared from the GL reaches 1531.1594%, the toughness reaches 12.315% MJ/m , the repairing efficiency reaches 103.62% after the polyurethane elastomer is repaired for 6 h at the normal temperature, and the repairing efficiency reaches 125.53% after the polyurethane elastomer is repaired for 2 h at the temperature of 80 DEG C. The prepared chain extender GL can be compounded with other reinforced chain extenders so as to be used, and the tensile strength and toughness of the polyurethane elastomer are further improved synergistically.
Discovery of a series of efficient, centrally efficacious bace1 inhibitors through structure-based drug design
Butler, Christopher R.,Brodney, Michael A.,Beck, Elizabeth M.,Barreiro, Gabriela,Nolan, Charles E.,Pan, Feng,Vajdos, Felix,Parris, Kevin,Varghese, Alison H.,Helal, Christopher J.,Lira, Ricardo,Doran, Shawn D.,Riddell, David R.,Buzon, Leanne M.,Dutra, Jason K.,Martinez-Alsina, Luis A.,Ogilvie, Kevin,Murray, John C.,Young, Joseph M.,Atchison, Kevin,Robshaw, Ashley,Gonzales, Cathleen,Wang, Jinlong,Zhang, Yong,Oneill, Brian T.
, p. 2678 - 2702 (2015/04/14)
The identification of centrally efficacious β-secretase (BACE1) inhibitors for the treatment of Alzheimers disease (AD) has historically been thwarted by an inability to maintain alignment of potency, brain availability, and desired absorption, distribution, metabolism, and excretion (ADME) properties. In this paper, we describe a series of truncated, fused thioamidines that are efficiently selective in garnering BACE1 activity without simultaneously inhibiting the closely related cathepsin D or negatively impacting brain penetration and ADME alignment, as exemplified by 36. Upon oral administration, these inhibitors exhibit robust brain availability and are efficacious in lowering central Amyloid β (Aβ) levels in mouse and dog. In addition, chronic treatment in aged PS1/APP mice effects a decrease in the number and size of Aβ-derived plaques. Most importantly, evaluation of 36 in a 2-week exploratory toxicology study revealed no accumulation of autofluorescent material in retinal pigment epithelium or histology findings in the eye, issues observed with earlier BACE1 inhibitors.