- Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): The effect of a terminal halogen substitution in the side-chain
-
Preliminary SAR studies on the side chain of a new class of antiviral nucleosides have shown that terminal substitution in the side-chain, with a halogen atom, lead to potent and highly specific anti-VZV agents. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Brancale, Andrea,McGuigan, Christopher,Andrei, Graciela,Snoeck, Robert,De Clercq, Erik,Balzarini, Jan
-
-
Read Online
- Well-Defined Biomimicking Brush-Polymer Self-Assemblies Revealing Cholesterol- and Phosphorylcholine-Enriched Surface
-
We have newly synthesized a series of well-defined brush polyethers bearing cholesterol (Chol) and phosphorylcholine (PC) moieties in various compositions which can mimic cell membrane. They were thermally stable up to at least 230 °C and soluble in common solvents, showing good solution processability. Excitingly, they all favorably self-assembled, forming multibilayer structures with 21 chain conformation; in comparison, the brush polyether bearing only PC-bristles formed orthorhombically packed cylinder (OPC) structure with 125 helical chain conformation. Such multibilayer structure formations could be driven by a strong self-assembling ability of the Chol-bristle in extended conformation; the multibilayer structure formation was further promoted by the presence of PC-bristles. The OPC structure formation could be driven by a lateral packing ability of the brush polymer chain in the helical confirmation resulted from the minimization of repulsive interactions in the neighbored zwitterionic PC-bristles. Because of such the self-assembling natures, all brush polymers always revealed Chol- and PC-enriched surface. Overall, all brush polyethers of this study successfully mimicked cell membrane features (Chol- and PC-surface based on self-assembling). They are very suitable for uses in the fields required cell membrane surface characteristics.
- Kim, Changsub,Kwon, Kyungho,Lee, Jongchan,Kim, Heesoo,Chae, Keun-Hwa,Ree, Moonhor
-
-
Read Online
- Total Synthesis and Structural Elucidation of Two Unusual Non-Methylene-Interrupted Fatty Acids in Ovaries of the Limpet Cellana toreuma
-
In our previous study, unusual odd-numbered dienoic acids with a terminal olefin were found as minor components in ovaries of the Japanese limpet Cellana toreuma, and the synthetic interests have been focused onto their structural confirmation and the inspection into their potential biological activity. Here, we describe an efficient and stereoselective total synthesis of two new unusual dienoic acids, 19:2?7,18 and 21:2?7,20, through a common pathway involving the strategic combination of alkyne-zipper reaction and Lindlar hydrogenation for the construction of their unique carbon chains. In our synthetic study, 2-propyn-1-ol was at first subjected to alkylation and alkyne-zipper reaction to form the two fragments, and the subsequent carbon chain elongation was achieved by the usual coupling reaction to obtain the C-19 and C-21 products bearing an internal acetylenic group. Then, the internal acetylenic group of these products was subjected to Lindlar hydrogenation to form a Z-alkenyl moiety, and the subsequent deprotection of the products was carried out under an acidic condition without isomerization of the internal Z-alkenyl group. Total synthesis of target fatty acids, 19:2?7,18 and 21:2?7,20, was finally accomplished by two-step oxidation of the resulting alcohols into carboxylic acids in a highly chemoselective manner, and the structures of these unusual natural fatty acids were finally elucidated by identifying the GC–MS spectra of the methyl esters of authentic and synthetic fatty acids.
- Shimada, Kazuaki,Sugawara, Ayako,Korenaga, Toshinobu,Kawashima, Hideki
-
p. 1019 - 1032
(2017/10/07)
-
- FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES
-
The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
Page/Page column 159; 160
(2016/01/25)
-
- Selective fluorescence labeling of lipids in living cells
-
Click chemistry in vivo: Three phosphatidic acid derivatives with alkyne groups in their fatty acid chains weresynthesized and incorporated into mammalian cell membranes. Cooper(l) catalyzed and strain-promoted azide-alkyne cycloaddition reactions were us
- Neef, Anne B.,Schultz, Carsten
-
supporting information; experimental part
p. 1498 - 1500
(2009/07/25)
-
- A simple, cost effective synthesis of E,Z-2,13-octadecadienyl acetate, a major sex pheromone component of lepidopteran pests
-
A simple, cost effective synthesis of E,Z-2,13-octadecadienyl acetate (1), a major sex pheromone component of many lepidopteran pests, has been achieved in optimum number of steps using cheaper raw meterials.The strategy provides the target compound in 43percent overall yield, and can be scaled up easily.
- Narasimhan, S.,Mohan, H.,Madhavan, S.
-
p. 531 - 534
(2007/10/02)
-
- Leukotriene antagonists
-
This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
- -
-
-
- THIOPHENYL ALKANOIC ACIDS USEFUL AS LEUKOTRIENE ANTAGONISTS
-
This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
- -
-
-