26410-96-8Relevant articles and documents
Synthesis and relaxometric characterization of a MRI Gd-based probe responsive to glutamic acid decarboxylase enzymatic activity
Napolitano, Roberta,Pariani, Giorgio,Fedeli, Franco,Baranyai, Zsolt,Aswendt, Markus,Aime, Silvio,Gianolio, Eliana
, p. 2466 - 2477 (2013/05/08)
Novel contrast agent based systems, which selectively visualize specific cells, e.g., neurons in the brain, would be of substantial importance for the fast developing field of molecular magnetic resonance imaging (MRI). We report here the synthesis and in vitro validation of a Gd(III)-based contrast agent designed to act as an MRI responsive probe for imaging the activity of the enzyme glutamic acid decarboxylase (GAD) present in neurons. Upon the action of the enzyme, the Gd(III) complex increases its hydration sphere and takes on a residual positive charge that promotes its binding to endogenous macromolecules. Both effects contribute in a synergic way to generate a marked relaxation enhancement, which directly reports enzyme activity and will allow activity detection of GAD positive cells in vitro and in vivo selectively.
HYDROXYMETHYL SUBSTITUTED DIHYDROISOXAZOLE DERIVATIVES USEFUL AS ANTIBIOTIC AGENTS
-
Page 79; 80, (2010/02/08)
Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, (I) R1a is NH(C=W)R5 or (a); W is O or S; R2 and R3 are for example H or F; R1 is for example hydrogen, or halogen; R5 is selected from hydrogen, (2-6C)alkyl (optionally substituted); R6 and R7 are independently selected from hydrogen, and (1-4C)alkyl (optionally substituted); wherein R4 is either a hydroxymethyl substituent on C-4' of the isoxazoline ring; or R4 is a hydroxymethyl substituent on C-5' of the isoxazoline ring and the stereochemistry at C-5' of the isoxazoline ring and at C-5 of the oxazolidinone ring is selected, such that the compound of formula (I) is a single diastereomer; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
Inhibitors of histone deacetylase
-
, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Synthesis of Haptens and Derivation of Monoclonal Antibodies for Immunoassay of the Phenylurea Herbicide Diuron
Karu, Alexander E.,Goodrow, Marvin H.,Schmidt, Douglas J.,Hammock, Bruce D.,Bigelow, Michael W.
, p. 301 - 309 (2007/10/02)
Diuron and related phenylurea herbicides and their metabolites are important candidates for sensitive and specific immunodetection.This paper describes a scheme for the the synthesis of two different types of phenylurea haptens for immunization and use as detecting conjugates in enzyme immunoassays (EIAs).The haptens were used to develop indirect and direct EIAs and to derive a panel of monoclonal antibodies (MAbs) with different specificities for diuron and its analogs.One of six possible combinations of hapten-spacer arm conjugates tested as immunizing and screening antigens resulted in an indirect competition EIA that was 100-2000-fold more sensitive than the others.The eight most sensitive MAbs had I50 values of 2-20 ppb for diuron.These MAbs gave two different patterns of cross-reactivities with monuron and linuron and negligible recognition of other arylurea herbicides.These MAbs and EIAs are potentially suitable for identification as well as detection of diuron, monuron, and linuron.
