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Your search keyword '"Vargas AJ"' showing total 3 results
Start Over Author "Vargas AJ" Publisher elsevier science ltd
3 results on '"Vargas AJ"'

1. Design, synthesis and identification of a new class of triarylmethyl amine compounds as inhibitors of apolipoprotein E production.

Author

Singh M, Schott JT, Leon MA, Granata RT, Dhah HK, Welles JA, Boyce MA, Oseni-Olalemi HS, Mordaunt CE, Vargas AJ, Patel NV, and Maitra S

Subjects
Amines chemical synthesis, Amines chemistry, Astrocytoma metabolism, Astrocytoma pathology, Cell Line, Tumor, Humans, Molecular Structure, Small Molecule Libraries chemistry, Amines pharmacology, Apolipoproteins E biosynthesis, Drug Design, Small Molecule Libraries chemical synthesis, Small Molecule Libraries pharmacology
Abstract

We have identified a new class of triarylmethyl amine compounds that can inhibit apolipoprotein E (apoE) production. ApoE is a cholesterol- and lipid-carrier protein implicated in aging, atherosclerosis, Alzheimer's Disease (AD), and other neurological and lipid-related disorders. Attenuation of apoE production is generally considered to be of therapeutic value. A majority of the apoE in the brain is produced by astrocytes. Here, we describe the design, synthesis, and biological screening of a small library of compounds that led to the identification of four triarylmethyl amines as potent inhibitors of apoE production in CCF-STTG1 astrocytoma cells., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Published
2012
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2. Synthesis of [(2S,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]-5-methylfuran-4-carboxylic acid derivatives: new leads as selective beta-galactosidase inhibitors.

Author

Moreno-Vargas AJ, Demange R, Fuentes J, Robina I, and Vogel P

Subjects
Animals, Carboxylic Acids chemical synthesis, Carboxylic Acids pharmacology, Enzyme Inhibitors pharmacology, Furans chemical synthesis, Furans pharmacology, Humans, Inhibitory Concentration 50, Pyrrolidines chemical synthesis, Pyrrolidines pharmacology, Structure-Activity Relationship, Enzyme Inhibitors chemical synthesis, beta-Galactosidase antagonists & inhibitors
Abstract

The preparation of [(2S,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]furan derivatives in a stereoselective route starting from D-glucose and ethyl acetoacetate is presented. Ethyl ester (6), N,N-diethylamide (7) and N-isopropylamide (8) have been tested towards 25 glycosidases. Ester (6) is a selective inhibitor of beta-galactosidases. The new compounds represent a new type of imino-C-nucleoside analogues.

Published
2002
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3. New leads for selective inhibitors of alpha-L-fucosidases. Synthesis and glycosidase inhibitory activities of [(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]furan derivatives.

Author

Robina I, Moreno-Vargas AJ, Fernández-Bolaños JG, Fuentes J, Demange R, and Vogel P

Subjects
Animals, Cattle, Drug Design, Drug Evaluation, Preclinical, Epididymis enzymology, Female, Furans chemistry, Inhibitory Concentration 50, Male, Placenta enzymology, Pregnancy, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, alpha-L-Fucosidase antagonists & inhibitors
Abstract

Readily derived from D-glucose, 5-[(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]-2-methyl-3-furoic esters and amides are selective and competitive inhibitors (K(i)> or = 3 microM) of alpha-L-fucosidase from bovine epididymis and from human placenta.

Published
2001
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