858981-15-4Relevant academic research and scientific papers
A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N -[3-[(Benzimidazol-2-yl)amino]propyl]amides
Keurulainen, Leena,Vahermo, Mikko,Puente-Felipe, Margarita,Sandoval-Izquierdo, Elena,Crespo-Fernández, Benigno,Guijarro-López, Laura,Huertas-Valentín, Leticia,De Las Heras-Due?a, Laura,Leino, Teppo O.,Siiskonen, Antti,Ballell-Pages, Lluís,Sanz, Laura M.,Casta?eda-Casado, Pablo,Jiménez-Díaz, M. Belén,Martínez-Martínez, María S.,Viera, Sara,Kiuru, Paula,Calderón, Félix,Yli-Kauhaluoma, Jari
supporting information, p. 4573 - 4580 (2015/06/25)
Malaria continues to be a major global health problem, being particularly devastating in the African population under the age of five. Artemisinin-based combination therapies (ACTs) are the first-line treatment recommended by the WHO to treat Plasmodium falciparum malaria, but clinical resistance against them has already been reported. As a consequence, novel chemotypes are urgently needed. Herein we report a novel, in vivo active, fast-acting antimalarial chemotype based on a benzimidazole core. This discovery is the result of a medicinal chemistry plan focused on improving the developability profile of an antichlamydial chemical class previously reported by our group. (Graph Presented).
Acidity of benzoic acids bearing the (CO)5Cr=CN(CH 3)2 group
Parik, Patrik,Kulhanek, Jiri,Ludwig, Miroslav,Wagner, Roman,Rotrekl, Ivan,Drahonovsky, Dusan,Meca, Ludek,Smidkova, Marketa,Tobrman, Tomas,Dvorak, Dalimil
experimental part, p. 4135 - 4138 (2011/01/03)
Benzoic acids 2a and 2b, bearing the (CO)5Cr=CN(CH 3)2 group in the p- and m-position, and the corresponding benzoic acids 2c and 2d, in which the rotation of the aminocarbene moiety was blocked by the presence of a methyl group, were prepared together with the corresponding N,N-dimethylamido acids 3a-d. The measurement of pKa values in EtOH and DMF revealed that the (CO)5Cr=CN(CH 3)2 group is a very weak electron acceptor (δp = 0; δm = 0.14). The restriction of the rotation of the aminocarbene moiety did not significantly influence its electronic properties. The obtained results are in accordance with earlier findings that the relatively strong acidity of carbene complexes bearing hydrogens at the ±-position to the carbene atom is due to the resonance stabilization of the anion.
THIAZOLE DERIVATIVE
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Page/Page column 136, (2010/11/23)
(Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic grou
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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Page/Page column 66-67, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
