کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1392278 | 1501127 | 2015 | 9 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis, bioassay, and QSAR study of bronchodilatory active 4H-pyrano[3,2-c]pyridine-3-carbonitriles Synthesis, bioassay, and QSAR study of bronchodilatory active 4H-pyrano[3,2-c]pyridine-3-carbonitriles](/preview/png/1392278.png)
• Pyrano[3,2-c]pyridines were synthesized in a facile synthetic approach.
• Bronchodilation properties of the pyrano[3,2-c]pyridines were reported.
• Many of the compounds synthesized exhibit promising activity compared with theophylline.
• A significant QSAR model was explored describing the bronchodilation activity.
A statistically significant QSAR model describing the bioactivity of bronchodilatory active 4H-pyrano[3,2-c]pyridine-3-carbonitriles (N = 41, n = 8, R2 = 0.824, R2cv = 0.724, F = 18.749, s2 = 0.0018) was obtained employing CODESSA-Pro software. The bronchodilatory active 4H-pyrano[3,2-c]pyridine-3-carbonitriles 17–57 were synthesized through a facile approach via reaction of 1-alkyl-4-piperidones 1–4 with ylidenemalononitriles 5–16 in methanol in the presence of sodium. The bronchodilation properties of 17–57 were investigated in vitro using isolated guinea pig tracheal rings pre-contracted with histamine (standard method) and compared with theophylline (standard reference). Most of the compounds synthesized exhibit promising bronchodilation properties especially, compounds 25 and 28.
A statistically significant QSAR model describing the bioactivity of bronchodilatory active 4H-pyrano[3,2-c]pyridine-3-carbonitriles.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 89, 7 January 2015, Pages 835–843