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Eight carbohydrate-pendant platinum(II) complexes have been synthesized from carbohydrate–diamine conjugates. d -Glucose, d -mannose, d -galactose, d -xylose, and l -glucose are attached to the dichloroplatinum(II) moiety by 1,3- or 1,2-diaminopropane chelates through with an O -glycoside bond....
A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human β 3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 ( 25 ), a potent β 3 full agonist ( K i =21 nM, 95% activation) with partial agonist (45%)...
Piperidinyl carboxylic acid-based derivatives were prepared as antagonists of the leukocyte cell adhesion process that is mediated through the interaction of the α 4 β 1 integrin (VLA-4, very late antigen 4) and the vascular cell adhesion molecule 1 (VCAM-1). Compounds 2a – h inhibited the...
New fluorescent ligands for adenosine receptors (ARs), obtained by the insertion, in the N 6 position of NECA, of NBD-moieties with linear alkyl spacers of increasing length, proved to possess a high affinity and selectivity for the A 3 subtype expressed in CHO cells. In fluorescence microscopy...
3α-Hydroxy-23,24-bisnorcholane spermidine and spermine carbamates 2 – 7 have been synthesized and their antimicrobial and hemolytic activities were evaluated. They exhibited excellent in vitro activities especially against methicillin-resistant Staphylococcus aureus .
A series of novel fluoroalkyl-containing tropane derivatives was synthesized, and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) were determined via competitive binding assays. Among these derivatives, the...
Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted β 3 selectivity. SAR elucidation established that highly selective β 3...
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