6853-58-3Relevant articles and documents
Azole-based non-peptidomimetic plasmepsin inhibitors
Kinena, Linda,Leitis, Gundars,Kanepe-Lapsa, Iveta,Bobrovs, Raitis,Jaudzems, Kristaps,Ozola, Vita,Suna, Edgars,Jirgensons, Aigars
, (2018/09/10)
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.
Odorless substitutes for foul-smelling thiols: Syntheses and applications
Node, Manabu,Kumar, Kamal,Nishide, Kiyoharu,Ohsugi, Shin-Ichi,Miyamoto, Tetsuo
, p. 9207 - 9210 (2007/10/03)
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.
Phenacenes: A family of graphite ribbons. 1. Syntheses of some [7]phenacenes by stilbene-like photocyclizations
Mallory, Frank B.,Butler, Kelly E.,Evans, Amanda C.,Mallory, Clelia W.
, p. 7173 - 7176 (2007/10/03)
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.