- Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors
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With the goal of improving metabolic stability and further enhancing FBPase inhibitory activity, a series of tricyclic 8H-indeno[1,2-d][1,3]thiazoles was designed and synthesized with the aid of structure-based drug design. Extensive SAR studies led to th
- Tsukada, Tomoharu,Takahashi, Mizuki,Takemoto, Toshiyasu,Kanno, Osamu,Yamane, Takahiro,Kawamura, Sayako,Nishi, Takahide
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scheme or table
p. 1004 - 1007
(2010/06/16)
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- Discovery of potent and orally active tricyclic-based FBPase inhibitors
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With the aim of exploring the effect of tricyclic-based FBPase inhibitors in cells and in vivo, a series of prodrugs of tricyclic phosphonates was designed and synthesized. Introducing prodrug moieties into tricyclic-based phosphonates led to the discover
- Tsukada, Tomoharu,Kanno, Osamu,Yamane, Takahiro,Tanaka, Jun,Yoshida, Taishi,Okuno, Akira,Shiiki, Takeshi,Takahashi, Mizuki,Nishi, Takahide
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experimental part
p. 5346 - 5351
(2010/09/05)
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- Anionic cyclizations of aromatic ester dithioacetals with facially biased α,β-unsaturated ketones
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Cyclopent-2-enones bearing a plane-nonsymmetric oxygen function on C-4 reacted efficiently with anions derived from aromatic ester dithioacetals to provide annulated products in a highly diastereoselective fashion. Whereas the anion of a dimethoxy aromati
- Morrison, Christopher F.,Stamp, Craig T.M.,Burnell, D. Jean
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supporting information; experimental part
p. 7021 - 7023
(2010/02/28)
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- The Dimerisation of Some 4-Hydroxyindenes
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The acid-catalysed dimerisation of the indenes (1)-(5), has been studied and a number of products isolated.The structure and stereochemistry of these compounds has been established by the use of crossed dimers, 13C-labelling, and 1H and 13C n.m.r. spectroscopy.
- Davis, Brian R.,Johnson, Stephen J.,Woodgate, Paul D.
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p. 2545 - 2554
(2007/10/02)
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- Synthetic Applications of Intramolecular Insertion in Arylcarbenes. VII. Aryl-Substituted Benzocycloalkenylidenes
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A series of benzo-fused cyclic carbenes, bearing suitably located alkoxy substituents in the phenyl ring, has been generated in the gas phase and pyrolysed at 250 deg/0.002-0.40 mm.In all cases, carbene insertion into the adjacent C-H bond (Bamford-Stevens insertion) occurs, either exclusively or predominantly, with up to 35percent 1,5 C-H insertion in the alkoxy sidechain to form peri-fused tricyclic heterocycles.These results are rationalized in terms of geometrical and electronic effects.
- Crow, Wilfrid D.,Engkaninan-Low, U.,Pang, Y. T.
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p. 1915 - 1924
(2007/10/02)
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