- Azole-based non-peptidomimetic plasmepsin inhibitors
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The spread of drug-resistant malaria parasites urges the search for new antimalarial drugs. Malarial aspartic proteases – plasmepsins (Plms) – are differentially expressed in multiple stages of the Plasmodium parasite's lifecycle and are considered as attractive drug targets. We report the development of novel azole-based non-peptidomimetic plasmepsin inhibitors that have been designed by bioisosteric substitution of the amide moiety in the Actelion amino-piperazine inhibitors. The best triazole-based inhibitors show submicromolar potency toward Plm II, which is comparable to that of the parent Actelion compounds. The new inhibitors can be used as a starting point for the development of a resistance-free antimalarial drug targeting the non-digestive Plm IX or X, which are essential for the malaria parasite life cycle.
- Kinena, Linda,Leitis, Gundars,Kanepe-Lapsa, Iveta,Bobrovs, Raitis,Jaudzems, Kristaps,Ozola, Vita,Suna, Edgars,Jirgensons, Aigars
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- 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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- Odorless substitutes for foul-smelling thiols: Syntheses and applications
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Several alkanethiols and p-alkylphenylmethanethiols were synthesized, and their odors were compared with those of ethanethiol and benzyl mercaptan by human and instrumental sensors. Among the various thiols analyzed, 1-dodecanethiol (1) and p-heptylphenylmethanethiol (3) were revealed to be odorless. 1-Dodecanethiol (1) has been used instead of ethanethiol for dealkylation of ethers, and p-heptylphenylmethanethiol (3) can replace benzyl mercaptan in the preparation of a 1,3-mercapto alcohol from an α,β-unsaturated ketone. These odorless thiols will greatly improve the physical environment of the researcher working with these foul-smelling compounds.
- Node, Manabu,Kumar, Kamal,Nishide, Kiyoharu,Ohsugi, Shin-Ichi,Miyamoto, Tetsuo
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p. 9207 - 9210
(2007/10/03)
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- Phenacenes: A family of graphite ribbons. 2. Syntheses of some [7]phenacenes and an [11]phenacene by stilbene-like photocyclizations
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It is proposed that members of the family of polycyclic aromatic compounds with an extended phenanthrene-like structural motif be designated as [n]phenacenes, where n is the number of fused benzene rings. [n]Phenacene molecules are related to layers of gr
- Mallory, Frank B.,Butler, Kelly E.,Evans, Amanda C.,Brondyke, Emilie J.,Mallory, Clelia W.,Yang, Changqing,Ellenstein, Aviva
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p. 2119 - 2124
(2007/10/03)
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- Phenacenes: A family of graphite ribbons. 1. Syntheses of some [7]phenacenes by stilbene-like photocyclizations
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The largest previously reported phenacene, the name we propose for the family of polycyclic aromatic compounds having fused benzene rings in an extended phenanthrene-like structural motif, contains only six rings ([6]phenacene). We have employed stilbene-like photocyclizations to synthesize the unsubstituted [7]phenacene, an extremely insoluble compound, as well as 2,13-di-n-pentyl[7]phenacene and 2,13-di-tert-butyl[7]phenacene, two alkyl-substituted derivatives with greatly improved solubilities.
- Mallory, Frank B.,Butler, Kelly E.,Evans, Amanda C.,Mallory, Clelia W.
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p. 7173 - 7176
(2007/10/03)
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- 1-(TRANS-4 prime -N-ALKYLCYCLOHEXYL)-2-(4 double prime -CYANOPHENYL)ETHANES - A NEW SERIES OF STABLE NEMATOGENS OF POSITIVE DIELECTRIC ANISOTROPY.
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The synthesis and some important properties of the 1-(trans-4 prime -n-alkylcyclohexyl)-2-(4 double prime -cyanophenyl)ethanes - where n-alkyl equals C//1 to C//7 - are described.
- Carr,Gray,McDonnell
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