کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365854 981575 2007 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists
چکیده انگلیسی

The preparation and structure–activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK1 antagonists in vitro and efficacious in vivo with minimal interactions with P450 liver enzymes. Oxadiazole analog 22 was determined to have excellent hNK1 binding affinity, functional activity, and a good PD response in vivo.

The preparation and structure–activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK1 antagonists in vitro and efficacious in vivo with minimal interactions with P450 liver enzymes. Oxadiazole 22 was determined to have excellent hNK1 binding affinity, functional activity, and a good PD response in vivo.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 19, 1 October 2007, Pages 5310–5315
نویسندگان
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