کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360993 | 981455 | 2011 | 15 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: A highly potent orally available CCR5 selective antagonist
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Based on the original spirodiketopiperazine design framework, further optimization of an orally available CCR5 antagonist was undertaken. Structural hybridization of the hydroxylated analog 4 derived from one of the oxidative metabolites and the new orally available non-hydroxylated benzoic acid analog 5 resulted in another potent orally available CCR5 antagonist 6a as a clinical candidate. Full details of a structure–activity relationship (SAR) study and ADME properties are presented.
Discovery of a new orally available CCR5 antagonist.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 13, 1 July 2011, Pages 4028–4042
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 13, 1 July 2011, Pages 4028–4042
نویسندگان
Rena Nishizawa, Toshihiko Nishiyama, Katsuya Hisaichi, Chiaki Minamoto, Masayuki Murota, Yoshikazu Takaoka, Hisao Nakai, Hideaki Tada, Kenji Sagawa, Shiro Shibayama, Daikichi Fukushima, Kenji Maeda, Hiroaki Mitsuya,