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A series of conformationally controlled 2-PAM derivatives were prepared from 2-acetylpyridine and 2,3-pyrido( b )cycloalkenones in two steps and their reactivities towards parathion poisoned AChE were evaluated. The most planar 2,3-pyrido( b )cyclohexanone oxime methiodide showed an activity...
The inhibitory activity of several crude drugs on α-glucosidases, which are the key enzymes for carbohydrate digestion and the prevention of diabetic complications, was investigated. Several crude drugs including Terminaliae Fructus, Mori Cortex Radicis, Caesalpiniae Lignum and Gyrophora...
A thymic stromal cell line, TFGD, was established from a thymic tumor mass developed spontaneously in p53 knock out. mouse, and was found to produce cytokines that could induce bone marrow hematopoietic stem cells (HSCs) to differentiate into macrophages. The cytokines produced by the TFGD line...
The diethyl ether extract of Isodon excisus var. coreanus exhibited significant inhibitory activity in aromatase assay. Bioactivity-guided fractionation of the extract led to the isolation of three active compounds: inflexin ( ent -1α-hydroxy-3β,6a-diacetoxykaur-16-en-11,15-dione) ( 1 ),...
The immunomodulating activity of a polysaccharide isolated from Morus alba (PMA) root bark was examined in murine splenic lymphocytes. PMA enhanced proliferation of splenic lymphocytes in a synergistic manner in the presence of mitogens. However, PMA suppressed primary IgM antibody production,...
(1′R, 2R)-, (1′R, 2S)-, (1′S, 2R)- and (1′S, 2S)-α-hydroxymetoprolol; (2R)- and (2S)- O -desmethylmetoprolol; and (2R)- and (2S)-metoprolol acid are major metabolites of (2R)-and (2S)-metoprolol, β-adrenergic antagonist. The focus of most chiral separation methods until now has been on...
To obtain the standard compounds of metoprolol for a pharmacokinetic study, a convenient synthetic procedure to prepare enantiomers of metoprolol ( 3a ) and its major metaboites, 2-4-(2-hydroxy-3-isopropylamino)propoxyphenylethanol ( 3b ) and 4-(2-hydroxy-3-isopropylamino) pro-poxyphenylacetic...
In most tissues, apoptosis plays a pivotal role in normal development and for regulating cell number, thus inappropriate apoptosis underlies a variety of diseases. Caspase-3 is one of a family of caspases that are mainly involved in the apoptotic signal transduction pathway, where caspase-3 acts...
L-3-Deoxymimosine-containing decapeptides were prepared for the development of protein tyrosine kinase (PTK) inhibitors. During the preparation of peptides, several side products were formed. Identification and determination of major peptides generated were reported.
A convenient pathway for synthesis of trans -metanicotine analogues was developed. trans -Metanicotine, a subtype(α4β2)-selective ligand for neuronal nicotinic acetylcholine receptor, is under clinical phase for Alzheimer’s disease. Zn-mediated allylation of allyl bromide and acetaldehyde...
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