کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8993366 | 1556389 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Non-imidazole histamine NO-donor H3-antagonists
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موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
Recently a series of H3-antagonists related to Imoproxifan was realised (I); in these products the oxime substructure of the lead was constrained in NO-donor furoxan systems and in the corresponding furazan derivatives. In this paper, a new series of compounds derived from I by substituting the imidazole ring with the ethoxycarbonylpiperazino moiety present in the non-imidazole H3-ligand A-923 is described. For all the products synthesis and preliminary pharmacological characterisation, as well as their hydrophilic-lipophilic balance, are reported. The imidazole ring replacement generally results in a decreased H3-antagonist activity with respect to the analogues of series I and, in some cases, induces relaxing effects on the electrically contracted guinea-pig ileum, probably due to increased affinity for other receptor systems.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Il Farmaco - Volume 60, Issues 6â7, JuneâJuly 2005, Pages 507-512
Journal: Il Farmaco - Volume 60, Issues 6â7, JuneâJuly 2005, Pages 507-512
نویسندگان
Paolo Tosco, Massimo Bertinaria, Antonella Di Stilo, Clara Cena, Roberta Fruttero, Alberto Gasco,