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1.
Inorg Chem ; 61(29): 11103-11109, 2022 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-35816337

RESUMEN

A new aluminosilicate zeolite, denoted EMM-28, has been successfully synthesized on a large scale using 1,1-(3,3-(1,3-phenylene)bis(propane-3,1-diyl))bis(1-methylpyrrolidinium) hydroxide as an organic structure directing agent (OSDA), which was scaled up to an ∼20 g scale with a yield of 77%. It crystallizes as thin plates (40-100 nm in thickness), and the corresponding powder X-ray diffraction (PXRD) pattern shows significant peak broadening which makes it insufficient for structure determination. Continuous rotation electron diffraction (cRED) data collected from 13 crystals were successfully used to solve and refine the structure of EMM-28. This illustrates that cRED data are capable of performing structure determination despite limited PXRD data quality. EMM-28 has a unique framework structure containing supercavities, >21 Šin size, connected by one-dimensional 10-ring channels. High-resolution transmission electron microscopy (HRTEM) confirmed the structure model. The structure of EMM-28 is related to several known zeolite structures with large cavities.

2.
Bioorg Med Chem Lett ; 18(18): 4929-31, 2008 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-18771916

RESUMEN

Norepinephrine and serotonin play an important role in a wide variety of biological processes and are implicated in a number of neurological disorders. A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones was designed and synthesized that displays potent norepinephrine reuptake inhibition while maintaining high selectivity (>100-fold) against the human serotonin and dopamine transporters.


Asunto(s)
Indoles/síntesis química , Indoles/farmacología , Inhibidores de la Captación de Neurotransmisores/síntesis química , Inhibidores de la Captación de Neurotransmisores/farmacología , Norepinefrina/antagonistas & inhibidores , Humanos , Indoles/química , Estructura Molecular , Inhibidores de la Captación de Neurotransmisores/química , Estereoisomerismo , Relación Estructura-Actividad
3.
J Med Chem ; 51(6): 1861-73, 2008 Mar 27.
Artículo en Inglés | MEDLINE | ID: mdl-18318463

RESUMEN

We have continued to explore the 3,3-dialkyl-5-aryloxindole series of progesterone receptor (PR) modulators looking for new agents to be used in female healthcare: contraception, fibroids, endometriosis, and certain breast cancers. Previously we reported that subtle structural changes with this and related templates produced functional switches between agonist and antagonist properties ( Fensome et al. Biorg. Med. Chem. Lett. 2002, 12, 3487; 2003, 13, 1317 ). We herein report a new functional switch within the 5-(2-oxoindolin-5-yl)-1 H-pyrrole-2-carbonitrile class of compounds. We found that the size of the 3,3-dialkyl substituent is important for controlling the functional response; thus small groups (dimethyl) afford potent PR antagonists, whereas larger groups (spirocyclohexyl) are PR agonists. The product from our optimization activities in cell-based systems and also for kinetic properties in rodents and nonhuman primates was 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1 H-indol-5-yl)-1-methyl-1 H-pyrrole-2-carbonitrile 27 (WAY-255348), which demonstrated potent and robust activity on PR antagonist and contraceptive end points in the rat and also in cynomolgus and rhesus monkeys including ovulation inhibition, menses induction, and reproductive tract morphology.


Asunto(s)
Diseño de Fármacos , Indoles/química , Indoles/síntesis química , Indoles/farmacología , Pirroles/química , Receptores de Progesterona/antagonistas & inhibidores , Administración Oral , Fosfatasa Alcalina/efectos de los fármacos , Animales , Relación Dosis-Respuesta a Droga , Femenino , Humanos , Macaca fascicularis , Macaca mulatta , Estructura Molecular , Ovulación/efectos de los fármacos , Oxindoles , Pirroles/síntesis química , Pirroles/farmacología , Ratas , Receptores de Progesterona/química , Estereoisomerismo , Relación Estructura-Actividad , Células Tumorales Cultivadas
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