- Making a difference on excited-state chemistry by controlling free space within a nanocapsule: Photochemistry of 1-(4-alkylphenyl)-3-phenylpropan-2-ones
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The free space within a reaction cavity plays a determining role during the excited-state reaction of 1-(4-alkylphenyl)-3-phenylpropan-2-ones included within a capsule formed by two molecules of a deep cavity cavitand. By controlling the free space within the reaction cavity through remote alkyl substitution on the reactant ketone it is possible to control the yield of the rearrangement product shown above.
- Sundaresan, Arun Kumar,Ramamurthy
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p. 3575 - 3578
(2008/02/12)
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- Benzylimidazolines as h5-HT(1B/1D) serotonin receptor ligands: A structure-affinity investigation
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Benzylimidazolines may represent a class of 5-HT(1D) ligands that has yet to be exploited. On the basis of a previous report that the 2- (substituted-benzyl)imidazoline α-adrenergic agonist oxymetazoline (8) binds with high affinity at calf brain 5-HT(1D) receptors, we explored the structure-affinity relationships of a series of related derivatives. Each of the aromatic substituents was removed and then reinstated in a systematic manner to determine the influence of the individual substituents on binding. It was found that all of the aromatic substituents of 8 act in concert to impart high affinity. However, although the 3-hydroxy group could be removed without significantly reducing affinity for h5-HT(1D) (i.e., human 5- HT(1Dα)) receptors, this modification reduced h5-HT(1B) (i.e., human 5- HT(1Dβ)) receptor affinity by nearly 50-fold. The 2,6-dimethyl groups also contribute to binding but seem to play a greater role for h5-HT(1B) binding than h5-HT(1D) binding. With the appropriate structural modifications, several compounds were identified that display 20- to > 100-fold selectivity for h5-HT(1D) versus h5-HT(1B) receptors. Preliminary functional data suggest that these compounds behave as agonists. Given that 5-HT(1D) agonists are currently being explored for their antimigraine action and that activation of h5-HT(1B) receptors might be associated with cardiovascular side effects, h5- HT(1D)selective agents may offer a new lead for the development of therapeutically efficacious agents.
- Law, Ho,Dukat, Malgorzata,Teitler, Milt,Lee, David K. H.,Mazzocco, Lucia,Kamboj, Raj,Rampersad, Vik,Prisinzano, Thomas,Glennon, Richard A.
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p. 2243 - 2251
(2007/10/03)
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- Coumarin derivative and use thereof
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The present invention provides compounds having 12-lipoxygenase inhibitory effect and medicines inhibiting 12-lipoxygenase selectively, and relates to novel coumarin derivatives and medicines containing the compounds as effective ingredients. Furthermore,
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- Stilbene derivative and stilbene analog derivative, and use thereof
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The present invention relates to a novel compound having a 12-lipoxygenase inhibitory effect, of the general formula (I), a precursor thereof, and a medicine containing the same, STR1 wherein R1 represents a hydrogen atom or a hydroxy group; on
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- Enzymes in organic synthesis 50. Probing the dimensions of the large hydrophobic binding region of the active site of pig liver esterase using substituted aryl malonate substrates
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The active side model reported recently for the synthetically useful enzyme pig liver esterase (PLE) permits the structural specificity and stereoselectivity of the enzyme to be interpreted and predicted for a wide range of substrates. The specifications
- Toone,Jones
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p. 1041 - 1052
(2007/10/02)
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