258 research outputs found
sj-pdf-1-chl-10.1177_17475198221079498 – Supplemental material for A stepwise lactol carbocyclisation to bridged ethers via a keto–acetal cascade
No full textSupplemental material, sj-pdf-1-chl-10.1177_17475198221079498 for A stepwise lactol carbocyclisation to bridged ethers via a keto–acetal cascade by Sean McCarthy and Charles M Marson in Journal of Chemical Research</p
Pteridine-2,4-diamine derivatives as radical scavengers and inhibitors of lipoxygenase that can possess anti-inflammatory properties
No full textBACKGROUND: Reactive oxygen species are associated with inflammation implicated in cancer, atherosclerosis and autoimmune diseases. The complex nature of inflammation and of oxidative stress suggests that dual-target agents may be effective in combating diseases involving reactive oxygen species. RESULTS: A novel series of N-substituted 2,4-diaminopteridines has been synthesized and evaluated as antioxidants in several assays. Many exhibited potent lipid antioxidant properties, and some are inhibitors of soybean lipoxygenase, IC50 values extending down to 100 nM for both targets. Several pteridine derivatives showed efficacy at 0.01 mmol/kg with little tissue damage in a rat model of colitis. 2-(4-methylpiperazin-1-yl)-N-(thiophen-2-ylmethyl)pteridin-4-amine (18f) at 0.01 mmol/kg exhibited potent anti-inflammatory activity (reduction by 41%). CONCLUSION: The 2,4-diaminopteridine core represents a new scaffold for lipoxygenase inhibition as well as sustaining anti-inflammatory properties
An asymmetric synthesis of aza analogues of the tricyclic skeleton of daphnane and the ABC ring system of phorbol
No full textAn asymmetric synthesis of aza analogues of the ABC ring system of phorbol and related compounds containing the 5-7-6-fused framework of daphnane involved construction of the central seven-membered ring by a regioselective reduction of a chiral imide and cyclization with trifluoromethanesulfonic acid. Subsequent demethylation and oxidative dearomatization of ring C afforded an enantiopure dienone 20 with the same relative and absolute configuration at the 9- and 10-positions of the phorbol skeleton
Synthesis of (3S,3S',4S,4S')-1,1'-ethylenedipyrrolidine-3,3',4,4'-tetraol and related diamino diols: donor-acceptor hydrogen-bonding motifs of the C-2 symmetric 3,4-dihydroxypyrrolidine unit
No full textEnantiopure 1,1'-ethylenedipyrrolidines possessing 3,4-disubstitution have been prepared from esters of L-(+)-tartaric acid. Although diacylation routes via the diacetoxypyrrolidin-2,5-diones were problematic, N,N-dialkylation protocols proved to be reliable and led to the synthesis of(3S,3S',4S,4S')-1,1'-ethylenedipyrrolidine-3,3',4,4'-tetraoi, (3R,3'S,4R,4'S)-3,4-diamino-1,1'-ethylenedipyrrolidine-3',4'-diol and (3R,3'R,4S,4'S)-3,3'-diamino-1,1'-ethylenedipyrrolidine-4,4'-diol. The tetraol possesses a crystal structure that exhibits an unusual zig-zag intermolecular pattern comprising a network of hydrogen bonds involving the terminal hydroxyl groups and a nitrogen atom of one of the pyrrolidine rings
ChemInform Abstract: Multicomponent and Sequential Organocatalytic Reactions: Diversity with Atom‐Economy and Enantiocontrol
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Reactions of carbonyl compounds with (monohalo) methyleniminium salts (vilsmeier reagents)
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