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Novel series of diaryl indenes and benzofurans have been shown to be potent and selective COX-2 inhibitors. A structure-activity relationship study suggests that the conversion of sulfones to sulfonamides affords potent, but slightly less selective COX-2 inhibitors, and that for benzofurans the...
Synthesis and in vitro activity of two novel conjugates ( 4 and 5 ) of desferrioxamine B, with nalidixic acid ( 2 ) and anthraquinone carboxylic acid ( 3 ), are described.
Several polyhydroxylated 3-(N-phenyl) carbamoly-2-iminochromene derivatives were synthesized and their inhibitory effects on tyrosine kinase p60 c-src were evaluated. The structure-activity relationship reveals that the positions of the hydroxylation on both the iminochromene ring and the...
The discovery of CP-161,242 (5-cyano-1-(3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl)benzimidazole), a potent, selective, orally active central serotonin (5-HT 1D ) agonist (IC 50 (binding) = 1.3 nM, EC 50 (inhibition of adenylate cyclase) = 42 pM) and benzodiazepine ligand ( IC 50 ( binding ) =...
Two constrained analogues ( 4a and 4b ) of both 4-DAMP ( 1 ) and spiro-DAMP ( 2 ) were designed, and their biological profiles at muscarinic receptor subtypes were assessed by functional and binding assays. It turned out that these constrained analogues display a modest, if any, M 2 /M 3...
1-(Indol-5-yl)pyrido(2,3-b)imidazoles and 1-(indol-5-yl)benzimidazoles ( 1 ) have been found to be unique, novel templates for potent benzodiazepine receptor affinity. The “molecular switch” for this activity lies in the imidazole N3 atom: replacement of this nitrogen for carbon (i.e., as in...
Selective methanolysis or dehydration followed by reduction of the 3-hydroxyglutamine residue of pneumocandin B 0 ( 1 ) or its dideoxy analog 5 (L-692,289) gave the methyl 3-hydroxyglutamate and 3-hydroxyornithine analogs 6 and 9 , respectively. Further derivatization of these analogs allowed a...
A new cyclic hexapeptide, dichotomin A, showing cell growth inhibitory activity, has been isolated from the roots of Stellaria dichotoma L. var. lanceolata Bge. and the structure and solid state conformation were elucidated by extensive 2D NMR, chemical degradation and X-ray analysis.
Acylsulphonamide analogues of the meta-tolylurea L-708,474 have been synthesised and evaluated as CCK B receptor antagonists. Such derivatives retain very high affinity and subtype selectivity for the CCK B receptor, and have good aqueous solubility. The ortho-tolyl acylsulphonamide L-736,309 is...
An attempt was made to synthesise calcineurin inhibitors using dual domain macrocyclic compounds that incorporated a FKBP12 binding domain together with a calcineurin recognition domain which had been designed by consideration of the relevant features of both FK506 and Cyclosporin A.
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