34099-62-2Relevant academic research and scientific papers
Preparation of a New Chiral Stationary Phase Based on Macrocyclic Amide Chiral Selector for the Liquid Chromatographic Chiral Separations
Sung, Ji Yeong,Choi, Seung Hyuck,Hyun, Myung Ho
, p. 253 - 258 (2016/02/26)
A new chiral stationary phase (CSP) based on macrocyclic amide receptor was prepared starting from (1R,2R)-1,2-diphenylethylenediamine. The new CSP was successfully applied to the resolution of various N-(substituted benzoyl)-α-amino amides with reasonably good separation factors and resolutions (α = 1.75 ~ 2.97 and RS = 2.89 ~ 6.82 for 16 analytes). The new CSP was also applied to the resolution of 3-substituted 1,4-benzodiazepin-2-ones and some diuretic chiral drugs including bendroflumethiazide and methylchlothiazide and metolazone. The resolution results for 3-substituted 1,4-benzodiazepin-2-ones and some diuretic chiral drugs were also reasonably good. Chirality 28:253-258, 2016.
New insight into the central benzodiazepine receptor-ligand interactions: Design, synthesis, biological evaluation, and molecular modeling of 3-substituted 6-phenyl-4 H -imidazo[1,5- a][1,4]benzodiazepines and related compounds
Anzini, Maurizio,Valenti, Salvatore,Braile, Carlo,Cappelli, Andrea,Vomero, Salvatore,Alcaro, Stefano,Ortuso, Francesco,Marinelli, Luciana,Limongelli, Vittorio,Novellino, Ettore,Betti, Laura,Giannaccini, Gino,Lucacchini, Antonio,Daniele, Simona,Martini, Claudia,Ghelardini, Carla,Di Cesare Mannelli, Lorenzo,Giorgi, Gianluca,Mascia, Maria Paola,Biggio, Giovanni
supporting information; experimental part, p. 5694 - 5711 (2011/10/08)
3-Substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds were synthesized as central benzodiazepine receptor (CBR) ligands. Most of the compounds showed high affinity for bovine and human CBR, their Ki values spanning from the low nanomolar to the submicromolar range. In particular, imidazoester 5f was able to promote a massive flow of 36Cl- in rat cerebrocortical synaptoneurosomes overlapping its efficacy profile with that of a typical full agonist. Compound 5f was then examined in mice for its pharmacological effects where it proved to be a safe anxiolytic agent devoid of the unpleasant myorelaxant and amnesic effects of the classical 1,4-benzodiazepines. Moreover, the selectivity of some selected compounds has been assessed in recombinant α1β 2γ2L, α2β1γ 2L, and α5β2γ2L human GABAA receptors. Finally, some compounds were submitted to molecular docking calculations along with molecular dynamics simulations in the Cromer's GABAA homology model.
Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents
Guandalini,Cellai,Laurenzana,Scapecchi,Paoletti,Romanelli
supporting information; experimental part, p. 5071 - 5074 (2009/05/30)
This study concerns the synthesis of new histone deacetylase inhibitors (HDACi) characterized by a 1,4-benzodiazepine ring used as the cap, joined through an amide function or a triple bond as connection units, to a linear alkyl chain bearing the hydroxamate function as Zn2+-chelating group. Biological tests performed in human acute promyelocytic leukemia NB4 cells showed that new hybrids can induce histone H3/H4 acetylation, growth arrest, and also apoptosis. Notably, chiral compounds exhibit stereoselective activity.
