213192-56-4Relevant academic research and scientific papers
β-alanine derivatives
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, (2008/06/13)
The invention relates to β-alanine derivatives of formula (I), wherein Q1, Q2, Q3, Q4, R1, R2, R3, R4, R5, R6and n have the meaning as disclosed
A one-pot synthesis of 3-amino-3-arylpropionic acids
Tan,Weaver
, p. 7449 - 7461 (2007/10/03)
3-Aminopropionic acids (β-amino acids) are biologically active compounds of interest in medicinal and pharmaceutical chemistry. Twenty-one 3-amino-3-arylpropionic acids were synthesized via a facile one-pot synthesis. In addition, a series of mechanistic studies have been performed to optimize the production of these β-amino acids. The reaction mechanism of this one-pot synthesis of β-amino acids, as well as the electronic effect of para-substitution and the influence of solvent polarity on the proposed reaction mechanism are discussed.
Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists
Sulyok,Gibson,Goodman,H?lzemann,Wiesner,Kessler
, p. 1938 - 1950 (2007/10/03)
The solid-phase synthesis of a low molecular weight RGD mimetic library is described. Activities of the compounds in inhibiting the interaction of ligands, vitronectin and fibrinogen, with isolated immobilized integrins αvβ3 and αIIbβ3 were determined in a screening assay. Highly active and selective nonpeptide αvβ3 integrin antagonists with regard to orally bioavailability were developed, based on the aza-glycine containing lead compound 1. An important variation is the substitution of the aspartic amide of 1 by an aromatic residue. Furthermore, different guanidine mimetics have been incorporated to improve the pharmacokinetic profile. Exchange of the β-amino acid NH by a methylene moiety in one set of RGD mimetics leads to the azacarba analogue compounds representing a novel peptidomimetic approach, which should increase the metabolic stability.
New aromatase inhibitors. Synthesis and biological activity of aryl- substituted pyrrolizine and indolizine derivatives
Sonnet, Pascal,Dallemagne, Patrick,Guillon, Jean,Enguehard, Cecile,Stiebing, Silvia,Tanguy, Julien,Bureau, Ronan,Rault, Sylvain,Auvray, Pierrick,Moslemi, Safa,Sourdaine, Pascal,Seralini, Gilles-Eric
, p. 945 - 955 (2007/10/03)
We report herein the design and the synthesis of some aryl-substituted pyrrolizine and indolizine derivatives, on the basis of a hypothetical pharmacophore structure designed to fit the catalytic site of the human cytochrome P450 aromatase. The in vitro b
