63214-58-4Relevant academic research and scientific papers
Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety
Lv, Kai,Tao, Zeyu,Liu, Qian,Yang, Lu,Wang, Bin,Wu, Shuo,Wang, Apeng,Huang, Menghao,Liu, Mingliang,Lu, Yu
, p. 1 - 8 (2018/04/02)
We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC 1 μg/
Design and synthesis of a hybrid series of potent and selective agonists of α7 nicotinic acetylcholine receptor
Nencini, Arianna,Castaldo, Cristiana,Comery, Thomas A.,Dunlop, John,Genesio, Eva,Ghiron, Chiara,Haydar, Simon,Maccari, Laura,Micco, Iolanda,Turlizzi, Elisa,Zanaletti, Riccardo,Zhang, Jean
, p. 401 - 418 (2014/04/17)
α7 nicotinic acetylcholine receptor agonists are promising therapeutic candidates for the treatment of cognitive impairment. As a follow up of our internal medicinal chemistry program we investigated a novel series of α7 nAChR agonists. Starting from molecular docking studies on two series of molecules recently developed in our laboratories, an alternative scaffold was designed attempting to combine the optimal features of these previously identified urea and pyrazole compounds. Based on our previous SAR knowledge and on predicted drug-like properties, a small library was synthesized in parallel manner, affording compounds with excellent α7 nAChR activity, selectivity and preliminary ADME profile.
MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
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, (2010/02/17)
Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
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Page/Page column 21, (2008/06/13)
Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
Synthesis and antihypertensive activity of some new quinazoline derivatives
Honkanen,Pippuri,Kairisalo,Nore,Karppanen,Paakkari
, p. 1433 - 1438 (2007/10/02)
A series of substituted 2-piperidino-4-amino-6,7-dimethoxyquinazolines was synthesized and screened as potential antihypertensive agents. The hypotensive effect of all the new compounds was studied after intravenous administrations in urethane-anesthetized normotensive rats. The furoylpiperazine moiety in the prazosin molecule could be replaced by a more stable substituted piperidine group without loss of the blood pressure lowering activity. However, the nature of the substituent profoundly influenced the hypotensive potency as well as the duration of the hypotensive action. Some of the new compounds were found to be as potent as prazosin. On the basis of potency and the duration of the hypotensive action in the anesthetized rats, five of the most promising compounds were selected for further studies. Each of these agents exerted an antihypertensive effect upon oral administrations in conscious spontaneously hypertensive rats. At small doses, the new compounds appeared to be somewhat less potent than prazosin, but at the higher doses of 10-100 μmol/kg, two of them appeared to be even more efficacious antihypertensive agents than prazosin.
