6479-47-6Relevant academic research and scientific papers
BIM-46174 fragments as potential ligands of G proteins
Küppers, Jim,Benkel, Tobias,Annala, Suvi,Schnakenburg, Gregor,Kostenis, Evi,Gütschow, Michael
supporting information, p. 1838 - 1843 (2019/11/02)
The 5,6,7,8-Tetrahydroimidazo[1,2-A]pyrazine derivative BIM-46174 has received attention as Gαq inhibitor. We conducted structural reductions to monocyclic and bicyclic substructures to explore the chemical space of BIM fragments and to gain insights into the pharmacophore of BIM-Type Gαq inhibitors. Two piperazin-2-one-containing fragments and a small library of bicyclic lactams featuring fused pyrazine and diazepine rings were synthesized and evaluated. The results of a second messenger-based cellular assay indicate that the entire BIM structure is required for efficient Gαq inhibition.
NOVEL SUBSTITUTED AMIDES OF TRITERPENE DERIVATIVES AS HIV INHIBITORS
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, (2017/02/28)
The present invention relates to compounds of novel substituted amides of triteripene derivatives of formula (I); or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, tautomers, stereoisomers, prodrugs, compositions or combination thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y, Z1, Z2, Z3 and formula (II) are as defined herein. The present invention also relates to,, and pharmaceutical compositions comprising compounds of formula (I) useful for the treatment of viral diseases and particularly HIV mediated diseases.
Etude de la stereochimie de la reaction de cycloaddition dipolaire-1,3 de quelques 5-phenyl-3,6-dihydro-2H-1,4-oxazin-2-ones avec les N-methyl et N-phenylmaleimides
Monnier, Karin,Schmitt, Gerard,Laude, Bernard,Mercier, Marie-France,Kubicki, Marek M.,Jannin, Michel
, p. 181 - 190 (2007/10/02)
Six derivatives of 5-phenyl-3,4-dihydro-2H-1,4-oxazin-2-ones 1 were synthetized from α-amino acids.These compounds are precursors of six-membered cyclic azomethine ylids involving one stereocenter.The 1,3-dipolar species react with N-methyl and N-phenylma
