20330-52-3Relevant 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.
Perenosins: A new class of anion transporter with anti-cancer activity
Van Rossom, Wim,Asby, Daniel J.,Tavassoli, Ali,Gale, Philip A.
supporting information, p. 2645 - 2650 (2016/03/05)
A new class of anion transporter named 'perenosins' consisting of a pyrrole linked through an imine to either an indole, benzimidazole or indazole is reported. The indole containing members of the perenosin family function as effective transmembrane Cl-/NO3- antiporters and HCl cotransporters in a manner similar to the prodigiosenes. The compounds reduce the viability of MDA-MB-231 and MCF-7.
Study of the Influence of Molecular Length on the Characteristics of the Ordered Smectic Phase.
Benattar,Levelut,Strzelecki
, p. 1233 - 1240 (2007/10/05)
Study of DTA and X-rays of p-phenyl-benzylidene-p'-alkylanilines of mesomorphic phases demonstrates the predominant role of the aliphatic chain length. In effect, it governs the appearance of the different phases; the correlation between layers decreases for greater chain lengths. The nonlinear variations of SmB layer thickness for these compounds shows clearly the importance of steric effects coupled with the molecular length with respect to the dipolar effect.