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A series of salvinorin A derivatives modified at the C(4) position were prepared and screened for binding and functional activities at the human κ-opioid receptor. Several selective κ-full agonists are reported.
New free radical scavengers 1 and 2 were isolated from the methanolic extract of the fruiting body of the medicinal mushroom Inonotus xeranticus , along with the known compounds phelligridin D, 3,4-dihydroxybenzaldehyde, and 3,4-dihydroxybenzoic acid. Their structures were established by...
We report the preparation of a phosphoramidon precursor 16 in 44% yield from H -phosphonate 15 and H 2 N-Leu-Trp-OEt 4 .
A series of N -(2-hydroxy-3-sulfonamidobenzene)- N ′-arylcyanoguanidines was prepared. In general, these compounds proved to be potent antagonists of CXCR2 while the selectivity versus CXCR1 ranged from non-selective to >200-fold.
Synthesis, assaying, and computational results are reported for new anti-HIV agents that exhibit high potency, low cytotoxicity, and promising pharmacological properties.
A novel compound, ( E )-4-phenyl-3-(pyridine-2-yl)but-2-en-1-ol, showing antiproliferative effect is reported.
Among the tested oxime derivatives, cyano- and morpholino-substituted analogue 4f at R 2 and R 3 had the highest potency with an IC 50 value of 0.05 μM in whole human plasma.
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