79574-62-2Relevant academic research and scientific papers
Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type i positive allosteric modulators of α7 nicotinic acetylcholine receptors
Hogenkamp, Derk J.,Ford-Hutchinson, Thomas A.,Li, Wen-Yen,Whittemore, Edward R.,Yoshimura, Ryan F.,Tran, Minhtam B.,Johnstone, Timothy B. C.,Bascom, Gavin D.,Rollins, Hannah,Lu, Lena,Gee, Kelvin W.
, p. 8352 - 8365 (2013)
A series of novel arylpyrid-3-ylmethanones (7a-aa) were designed as modulators of α7 nicotinic acetylcholine receptors (nAChRs). The methanones were found to be type I positive allosteric modulators (PAMs) of human α7 nAChRs expressed in Xenopus ooctyes. Structure-activity relationship (SAR) studies resulted in the identification of compound 7v as a potent and efficacious type I PAM with maximum modulation of a nicotine EC 5 response of 1200% and EC50 = 0.18 μM. Compound 7z was active in reversing the effect of scopolamine in the novel object recognition (NOR) paradigm with a minimum effective ip dose of 1.0 mg/kg (2.7 μmol/kg). This effect was blocked by the selective α7 nAChR antagonist methyllycaconitine (MLA). These compounds are potent type I positive allosteric modulators of α7 nAChRs that may have therapeutic value in restoring impaired sensory gating and cognitive deficits in schizophrenia and Alzheimer's disease.
Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): Pyridodiazepine amines
Geng, Bolin,Basarab, Gregory,Comita-Prevoir, Janelle,Gowravaram, Madhusudhan,Hill, Pamela,Kiely, Andrew,Loch, James,MacPherson, Lawrence,Morningstar, Marshall,Mullen, George,Osimboni, Ekundayo,Satz, Alexander,Eyermann, Charles,Lundqvist, Tomas
scheme or table, p. 930 - 936 (2009/09/06)
An SAR study of an HTS screening hit generated a series of pyridodiazepine amines as potent inhibitors of Helicobacter pylori glutamate racemase (MurI) showing highly selective anti-H. pylori activity, marked improved solubility, and reduced plasma protei
PYRIDINYLMORPHOLINE DERIVATIVES
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Page/Page column 43, (2008/06/13)
The invention relates to compounds of formula (I); wherein R, R1, R2 and X are as defined herein, their preparation and their use as pharmaceuticals.
TREATMENT OF PERVASIVE DEVELOPMENTAL DISORDERS WITH NOREPINEPHRINE REUPTAKE INHIBITORS
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Page/Page column 260-261, (2010/02/11)
Provided are methods and medicaments for treating a Pervasive Developmental Disorder, comprising administering to a patient in need of such treatment an effective amount of a selective norepinephrine reuptake inhibitor.
TREATMENT OF HOT FLASHES, IMPULSE CONTROL DISORDERS AND PERSONALITY CHANGE DUE TO A GENERAL MEDICAL CONDITION
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Page/Page column 258-259, (2010/02/12)
Selective norepinephrine reuptake inhibitors are useful for the prevention or treatment of hot flashes, vasomotor symptoms, impulse control disorders or personality change due to a general medical condition.
Investigation of an alternative route to ZD3638 and cost-benefit analysis comparison of raw materials with the previous route
Moseley, Jonathan D.,Moss, William O.,Welham, Matthew J.
, p. 491 - 497 (2013/09/07)
A convergent synthesis to ZD3638 was proposed starting with alternative raw materials. A cost-benefit analysis for the new route was performed which demonstrated that significant savings in raw materials costs could be made over the previous linear sequence. The convergent route was then proved in principle by experimental work. LiTMP was shown to be a superior base to LDA in the modified lithiation reaction.
METALLATION REGIOSELECTIVE EN SERIE PYRIDINIQUE: SYNTHESE ORIGINALE D'AMINO-2-AROYL 3-PYRIDINES
Guengoer, Timur,Marsais, Francis,Queguiner, Guy
, p. 139 - 150 (2007/10/02)
Lithium diisopropylamide reacts with 2-fluoropyridine at low temperature: regioselectivity is excellent and metallation occurs without side reactions such as nucleophilic attack. 2-Fluoro-3-lithiopyridine is formed and with aldehydes it gives the correspo
