國家衛生研究院 NHRI:Item 3990099045/3084
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    题名: Synthesis, beta-adrenergic receptor binding and antihypertensive potential of vanillin-derived phenoxypropanolamines
    作者: Coumar, MS;Jindal, DP;Bruni, G;Massarelli, P;Singh, R;Sharma, AK;Nandakumar, K;Bodhankar, SL
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: Synthesis of vanillin-derived phenoxypropanolamines is carried out by condensing 4-hydroxy-3-methoxybenzaldehyde (vanillin) 1 with epichlorohydrin, followed by treatment with iso-propylamine or tert-butylamine to open the epoxy ring. Percentage inhibition of [H-3]dihydroalprenolol binding to both beta(1)- and beta(2)-adrenergic receptors by the newly synthesized compounds is assessed in vitro using turkey erythrocyte membrane (PI) and lung homogenate of rats A). Formyl derivatives 8 and 9 showed maximum inhibitory effect in binding assay and are non-selective similar to propranolol. On the other-hand, aldoxime compounds 10 and 11 have preference for PI-adrenergic receptors similar to atenolol. Also four of the compounds 8-11 are evaluated for their anti-hypertensive potential, in left renal artery ligation and fructose induced hypertension models. 4-(3-tert-Butylamino-2-hydroxy-propoxy)-3-methoxy-benzaldehydeoxime 11 shows antihypertensive effect better than propranolol.
    关键词: Chemistry, Organic
    日期: 2008-06
    關聯: Indian Journal of Chemistry Section B: Organic Chemistry Including Medicinal Chemistry. 2008 Jun;47(6):903-909.
    Link to: http://www.niscair.res.in/ScienceCommunication/ResearchJournals/rejour/IJCB/ijcb2k8/ijcb_jun08.asp
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000256931600003
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=48249148729
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