- Synthesis and antioxidant activity of 4-[2-(3,5-dimethoxyphenyl)ethenyl]-1, 2-benzenediol, a metabolite of Sphaerophysa salsula
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4-[2-(3,5-Dimethoxyphenyl)ethenyl]-1,2-benzenediol (7), a stilbene isolated from Sphaerophysa salsula, was synthesized from 3,4-dihydroxybenzaldehyde (1) in five steps in an overall yield of 33%. The spectral data for synthetic 7 are in good agreement with those of the natural product. Hydroxystilbene 7 showed potent antioxidative activity.
- Venkateswarlu, Somepalli,Satyanarayana, Boyina,Sureshbabu, Chillara V.,Subbaraju, Gottumukkala V.
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- Organocatalytic regioselective Michael additions of cyclic enones via asymmetric phase transfer catalysis
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The regioselective Michael addition of 2-cyclohexenone and to other enones under the PTC-conditions was investigated. If no other Michael acceptors were present treatment of 2-cyclohexenone under PTC conditions afforded the dimerization product. The enant
- Ceccarelli, Roberto,Insogna, Susanna,Bella, Marco
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p. 4281 - 4284
(2008/09/18)
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- Substituted γ-phenyl-Δ-lactams and uses related thereto
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γ-Phenyl-substituted Δ-lactams are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
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- Compound
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There is provided a compound of Formula I 1 wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C═O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.
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Page/Page column 44
(2008/06/13)
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- Substituted gamma-phenyl-delta-lactams and uses related thereto
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gamma-Phenyl-substituted Delta-lactams are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
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- New optically active 2H-azirin-3-amines as synthons for enantiomerically pure 2,2-disubstituted glycines: Synthesis of synthons for Tyr(2Me) and Dopa(2Me), and their incorporation into dipeptides
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The synthesis of novel unsymmetrically 2,2-disubstituted 2H-azirin-3-amines with chiral auxiliary amino groups is described. Chromatographic separation of the mixture of diastereoisomers yielded (1′R,2S)-2a,b and (1′R.2R)-2a,b (c.f. Scheme 1 and Table 1), which are synthons for (S)- and (R)-2-methyltyrosine and 2-methyl-3′,4′-dihydroxyphenylalanine. Another new synthon 2c, i.e., a synthon for 2-(azidomethyl)alanine, was prepared but could not be separated into its pure diastereoisomers. The reaction of 2 with thiobenzoic acid, benzoic acid, and the amino acid Fmoc-Val-OH yielded the monothiodiamides 11, the diamides 12 (cf. Scheme 3 and Table 3), and the dipeptides 13 (cf. Scheme 4 and Table 4), respectively. From 13, each protecting group was removed selectively under standard conditions (cf. Schemes 5-7 and Tables 5-6). The configuration at C(2) of the amino acid derivatives (1R,1′R)-11a, (1R,1′R)-11b, (1S,1′R)-12b, and (1R,1′R)-12b was determined by X-ray crystallography relative to the known configuration of the chiral auxiliary group.
- Brun, Kathrin A.,Linden, Anthony,Heimgartner, Heinz
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p. 3422 - 3443
(2007/10/03)
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- Substituted γ-phenyl-Δ-lactones and analogs thereof and uses related thereto
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γ-Phenyl-substituted Δ-lactones and analogs thereof, including lactams, are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
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- Synthesis and anti-HIV activity of dibenzylbutyrolactone lignans
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Five optically active dibenzylbutyrolactone lignans were synthesized through a lipase-catalyzed transesterification route and evaluated for their inhibitory activity against HIV-1 replication in acutely infected H9 cells. Compounds 1 and 2 demonstrated anti-HIV replication activity with an EC50 values of 2.2 and 0.16 μg/ml and a therapeutic index values of 9.1 and 5, respectively. Structure-antiviral activity relationships are discussed.
- Yang, Li-Ming,Lin, Shwu-Jiuan,Yang, Tsang-Hsiung,Lee, Kuo-Hsiung
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p. 941 - 944
(2007/10/03)
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- Synthesis and Protein-Tyrosine Kinase Inhibitory Activity of Polyhydroxylated Stilbene Analogues of Piceatannol
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A series of hydroxylated trans-stilbene related to the antileukemic natural product trans-3,3',4,5'-tetrahydroxy stilbene (piceatannol) (1) has been prepared and tested for inhibition of the lymphoid cell lineage-specific protein-tyrosine kinase p56lck, which plays an important role in lymphocyte proliferation and immune function.A number of the analogues displayed enhanced enzyme inhibitory activity relative to the natural product.Reduction of the double bond bridging the two aromatic rings and benzylation of the phenolic hydroxyl groups was found to decrease activity significantly.The most potent compounds in the series proved to be trans-3,3',5,5'-tetrahydroxystilbene, trans-3,3',5-trihydroxystilbene, and trans-3,4,4'-trihydroxystilbene.
- Thakkar, Kshitij,Geahlen, Robert L.,Cushman, Mark
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p. 2950 - 2955
(2007/10/02)
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