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Novel diarylheptanoids as inhibitors of TNF-α production.
Compounds 4i, 5b, 5d, and 5g significantly inhibit lipopolysaccharide (LPS)-induced TNF-α production from human peripheral blood mononuclear cells in a dose-dependent manner and indicate that these compounds may have potential therapeutic implications for T NF-α-mediated auto-immune/inflammatory disorders. Expand
Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.
Thiazolyl-phthalazinone acetamide was identified as a potential glucose uptake modulator and was superior to rosiglitazone under similar experimental conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold. Expand
Improves Synthesis of (±)-Praeruptorin A and Other Khellactone Esters by Solvent-free DCC Reactions
Esters of 4'-acetylkhellactone such as (+)-praeruptorin A (2) were synthesised in considerably improved yields through use of a low tempeature solvent-free DCC esterification reaction
A novel entry into 1,2,3,4,5,6-hexahydro-3-benzazocine-4,6-dione and 2-substituted-2,5,6,7-tetrahydro-4-benzazonine-1,3-(4H)-dione
Abstract 2-Substituted-1,2,3,4,5,6-hexahydro-3-benzazocine-4, 6-diones(1a-d) and 2-methoxy-2,5,6,7-tetrahydro-4-benzazonine-1,3-dione 8 were synthesized through an oxidative ring expansion reactionExpand
Synthesis of 1,4‐disubstituted quinolizidines
Two 9,11-seco-aphylline derivatives and four 4-substitutedimino-1-carbethoxyquinolizidines were synthesized. Conformational assignments of the predominant isomers were derived from spectral data.
HL 752: a potent and long-acting antispasmodic agent.
Of the compounds synthesised, HL 752 showed the most potent and long-lasting antispasmodic activity and was selected as the candidate for clinical development. Expand